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Genentech inc cbp/ep300 bromodomain inhibitors gne-781
Cbp/Ep300 Bromodomain Inhibitors Gne 781, supplied by Genentech inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/gne-781/gne+781/pm40156557-67-10-25
Average 90 stars, based on 1 article reviews
cbp/ep300 bromodomain inhibitors gne-781 - by Bioz Stars, 2026-09
90/100 stars

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Related Articles

Activation Assay:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Luciferase:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Quantitative RT-PCR:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Expressing:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Inhibition:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Histopathology:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Immunohistochemistry:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Western Blot:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Recombinant:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Chromatin Immunoprecipitation:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

RNA Sequencing Assay:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Multiple Displacement Amplification:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.

Software:

Article Title: Combined Targeting of the BRD4–NUT–p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734
Article Snippet: The authors thankKarenGascoigne (Genentech Inc.) for sharing GNE-781 with us.We thankDana-Farber/Harvard Cancer Center in Boston, MA, for the use of the Specialized Histopathology Core, which provided histology and IHC service.

Article Title: Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters
Article Snippet: Where required, cells were treated with 1.2 nM 4SC202 (Selleckchem), 100 nM A485 (Selleckchem), 100 nM GNE-781 ( ; kindly supplied by Karen Gascoigne, Genentech) or vehicle (DMSO) for one hour prior to induction with EGF.

Article Title: Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Article Snippet: BioXcell Cat# BP0090 Biological Samples Human healthy PBMCs (under protocols reviewed and approved by the Western Institutional Review Board) Genentech Protocol: CEHS-CP 307.2 Chemicals, Peptides, and Recombinant Proteins CBP/EP300-BRDi Genentech GNE-781 Deposited Data ChIP-seq and RNA-seq GEO Repository GSE124333 Experimental Models: Cell Lines MDA-MB-231 X1 (Homo sapiens; breast adenocarcinoma) Genentech GNE_ICVV CT26.WT (Mus musculus, colon carcinoma) ATCC Cat# CRL2638 Experimental Models: Organisms/Strains BALB/c mice Charles River Laboratories Cat# BALB/cAnNCrl SCID beige mice Charles River Laboratories Cat# CB17.Cg-PrkdcscidLystbg-J/Crl Software and Algorithms GraphPad prism software GraphPad version 6 Flowjo FlowJo, LLC Version 10.0.8r1 MATLAB MathWorks Cat# R2017b

Article Title: Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734
Article Snippet: The authors thank Karen Gascoigne (Genentech Inc., South San Francisco, CA) for sharing GNE-781 with us.

Article Title: Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Article Snippet: GNE-781, the molecule used in the current study, is a small-molecule 1 Safety Assessment, Genentech, Inc, South San Francisco, CA, USA 2 Vet Path Services, Inc, Mason, OH, USA 3 Medicinal Chemistry, Genentech, Inc, South San Francisco, CA, USA 4 Terns Pharmaceuticals, San Mateo, CA, USA 5 Department of Drug Metabolism and Pharmacology, Genentech, Inc, South San Francisco, CA, USA 6 Department of Pathology, Genentech, Inc, South San Francisco, CA USA Corresponding Author: Jonathan Maher, 1 DNA Way, MS 59, South San Francisco, CA 94080, USA.



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(A) Schematic of CBP/p300 domains and structures of relevant <t>inhibitors</t> <t>GNE-781</t> (bromodomain), A-485 (catalytic KAT domain), and degrader dCBP-1 (left); cancer cell line panel used for comparative viability profiling (middle); and quantitative dose-response metrics derived from 5-day viability assay (right). (B) Compiled and overlaid dose-response curves across 300 cell lines for dCBP-1 (left), GNE-781 (middle), and A-485 (right). Each cell line was screened in duplicate; for clarity, a single replicate for each cell line is shown. (C) Quantification of dose-response IC 50 , area under the curve (AUC), Hill slope ( HS ), and maximum effect ( E max ); each dot represents the mean value for each cell line in the screen ( n = 2 replicates per cell line); black line within each plot represents mean value across 300 cell lines. For IC 50 , if 50% inhibition was not determined within dose range tested, value was assigned at 100×the maximum dose tested; **** p < 0.0001, two-tailed paired t test; ns , not significant. (D) Average AUC values for each cell line categorized by lineage; gray bar within each plot represents mean value for each drug within lineage. (E) IC 50 values for each lymphoid cell line in screen. MM, multiple myeloma; B-ALL, B cell acute lymphoblastic leukemia; DLBCL/CLL, diffuse large B cell lymphoma/chronic lymphocytic leukemia; MCL, mantle cell lymphoma; HL, Hodgkin’s lymphoma; T-ALL, T cell acute lymphoblastic leukemia; and TCL, T cell lymphoma; values represent mean of two replicate experiments. (F) IC 50 values for most sensitive non-lymphoid cell lines in screen. RMS, rhabdomyosarcoma; MRT, malignant rhabdoid tumor; PCa, prostate cancer; NET, neuroendocrine tumor; NB, neuroblastoma; HCC, hepatocellular carcinoma; BrCa, breast cancer; and SCLC, small cell lung cancer; values represent mean of two replicate experiments. See also .
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(A) Schematic of CBP/p300 domains and structures of relevant <t>inhibitors</t> <t>GNE-781</t> (bromodomain), A-485 (catalytic KAT domain), and degrader dCBP-1 (left); cancer cell line panel used for comparative viability profiling (middle); and quantitative dose-response metrics derived from 5-day viability assay (right). (B) Compiled and overlaid dose-response curves across 300 cell lines for dCBP-1 (left), GNE-781 (middle), and A-485 (right). Each cell line was screened in duplicate; for clarity, a single replicate for each cell line is shown. (C) Quantification of dose-response IC 50 , area under the curve (AUC), Hill slope ( HS ), and maximum effect ( E max ); each dot represents the mean value for each cell line in the screen ( n = 2 replicates per cell line); black line within each plot represents mean value across 300 cell lines. For IC 50 , if 50% inhibition was not determined within dose range tested, value was assigned at 100×the maximum dose tested; **** p < 0.0001, two-tailed paired t test; ns , not significant. (D) Average AUC values for each cell line categorized by lineage; gray bar within each plot represents mean value for each drug within lineage. (E) IC 50 values for each lymphoid cell line in screen. MM, multiple myeloma; B-ALL, B cell acute lymphoblastic leukemia; DLBCL/CLL, diffuse large B cell lymphoma/chronic lymphocytic leukemia; MCL, mantle cell lymphoma; HL, Hodgkin’s lymphoma; T-ALL, T cell acute lymphoblastic leukemia; and TCL, T cell lymphoma; values represent mean of two replicate experiments. (F) IC 50 values for most sensitive non-lymphoid cell lines in screen. RMS, rhabdomyosarcoma; MRT, malignant rhabdoid tumor; PCa, prostate cancer; NET, neuroendocrine tumor; NB, neuroblastoma; HCC, hepatocellular carcinoma; BrCa, breast cancer; and SCLC, small cell lung cancer; values represent mean of two replicate experiments. See also .
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(A) Schematic of CBP/p300 domains and structures of relevant <t>inhibitors</t> <t>GNE-781</t> (bromodomain), A-485 (catalytic KAT domain), and degrader dCBP-1 (left); cancer cell line panel used for comparative viability profiling (middle); and quantitative dose-response metrics derived from 5-day viability assay (right). (B) Compiled and overlaid dose-response curves across 300 cell lines for dCBP-1 (left), GNE-781 (middle), and A-485 (right). Each cell line was screened in duplicate; for clarity, a single replicate for each cell line is shown. (C) Quantification of dose-response IC 50 , area under the curve (AUC), Hill slope ( HS ), and maximum effect ( E max ); each dot represents the mean value for each cell line in the screen ( n = 2 replicates per cell line); black line within each plot represents mean value across 300 cell lines. For IC 50 , if 50% inhibition was not determined within dose range tested, value was assigned at 100×the maximum dose tested; **** p < 0.0001, two-tailed paired t test; ns , not significant. (D) Average AUC values for each cell line categorized by lineage; gray bar within each plot represents mean value for each drug within lineage. (E) IC 50 values for each lymphoid cell line in screen. MM, multiple myeloma; B-ALL, B cell acute lymphoblastic leukemia; DLBCL/CLL, diffuse large B cell lymphoma/chronic lymphocytic leukemia; MCL, mantle cell lymphoma; HL, Hodgkin’s lymphoma; T-ALL, T cell acute lymphoblastic leukemia; and TCL, T cell lymphoma; values represent mean of two replicate experiments. (F) IC 50 values for most sensitive non-lymphoid cell lines in screen. RMS, rhabdomyosarcoma; MRT, malignant rhabdoid tumor; PCa, prostate cancer; NET, neuroendocrine tumor; NB, neuroblastoma; HCC, hepatocellular carcinoma; BrCa, breast cancer; and SCLC, small cell lung cancer; values represent mean of two replicate experiments. See also .
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Image Search Results


(A) Schematic of CBP/p300 domains and structures of relevant inhibitors GNE-781 (bromodomain), A-485 (catalytic KAT domain), and degrader dCBP-1 (left); cancer cell line panel used for comparative viability profiling (middle); and quantitative dose-response metrics derived from 5-day viability assay (right). (B) Compiled and overlaid dose-response curves across 300 cell lines for dCBP-1 (left), GNE-781 (middle), and A-485 (right). Each cell line was screened in duplicate; for clarity, a single replicate for each cell line is shown. (C) Quantification of dose-response IC 50 , area under the curve (AUC), Hill slope ( HS ), and maximum effect ( E max ); each dot represents the mean value for each cell line in the screen ( n = 2 replicates per cell line); black line within each plot represents mean value across 300 cell lines. For IC 50 , if 50% inhibition was not determined within dose range tested, value was assigned at 100×the maximum dose tested; **** p < 0.0001, two-tailed paired t test; ns , not significant. (D) Average AUC values for each cell line categorized by lineage; gray bar within each plot represents mean value for each drug within lineage. (E) IC 50 values for each lymphoid cell line in screen. MM, multiple myeloma; B-ALL, B cell acute lymphoblastic leukemia; DLBCL/CLL, diffuse large B cell lymphoma/chronic lymphocytic leukemia; MCL, mantle cell lymphoma; HL, Hodgkin’s lymphoma; T-ALL, T cell acute lymphoblastic leukemia; and TCL, T cell lymphoma; values represent mean of two replicate experiments. (F) IC 50 values for most sensitive non-lymphoid cell lines in screen. RMS, rhabdomyosarcoma; MRT, malignant rhabdoid tumor; PCa, prostate cancer; NET, neuroendocrine tumor; NB, neuroblastoma; HCC, hepatocellular carcinoma; BrCa, breast cancer; and SCLC, small cell lung cancer; values represent mean of two replicate experiments. See also .

Journal: Cell reports

Article Title: An orally active dual CBP/p300 degrader targets core dependencies of multiple myeloma

doi: 10.1016/j.celrep.2026.117464

Figure Lengend Snippet: (A) Schematic of CBP/p300 domains and structures of relevant inhibitors GNE-781 (bromodomain), A-485 (catalytic KAT domain), and degrader dCBP-1 (left); cancer cell line panel used for comparative viability profiling (middle); and quantitative dose-response metrics derived from 5-day viability assay (right). (B) Compiled and overlaid dose-response curves across 300 cell lines for dCBP-1 (left), GNE-781 (middle), and A-485 (right). Each cell line was screened in duplicate; for clarity, a single replicate for each cell line is shown. (C) Quantification of dose-response IC 50 , area under the curve (AUC), Hill slope ( HS ), and maximum effect ( E max ); each dot represents the mean value for each cell line in the screen ( n = 2 replicates per cell line); black line within each plot represents mean value across 300 cell lines. For IC 50 , if 50% inhibition was not determined within dose range tested, value was assigned at 100×the maximum dose tested; **** p < 0.0001, two-tailed paired t test; ns , not significant. (D) Average AUC values for each cell line categorized by lineage; gray bar within each plot represents mean value for each drug within lineage. (E) IC 50 values for each lymphoid cell line in screen. MM, multiple myeloma; B-ALL, B cell acute lymphoblastic leukemia; DLBCL/CLL, diffuse large B cell lymphoma/chronic lymphocytic leukemia; MCL, mantle cell lymphoma; HL, Hodgkin’s lymphoma; T-ALL, T cell acute lymphoblastic leukemia; and TCL, T cell lymphoma; values represent mean of two replicate experiments. (F) IC 50 values for most sensitive non-lymphoid cell lines in screen. RMS, rhabdomyosarcoma; MRT, malignant rhabdoid tumor; PCa, prostate cancer; NET, neuroendocrine tumor; NB, neuroblastoma; HCC, hepatocellular carcinoma; BrCa, breast cancer; and SCLC, small cell lung cancer; values represent mean of two replicate experiments. See also .

Article Snippet: GNE-781 , MedChem Express , Cat# HY-108696; CAS: 1936422-33-1.

Techniques: Derivative Assay, Viability Assay, Inhibition, Two Tailed Test

(A) Immunoassay measurements of CBP, p300, and BRD4 levels with dCBP-30 (top) or dCBP-1 (bottom) dose-response treatments with 4 h drug exposure in MM1.S cells; vinculin levels shown as loading controls. (B) Time-course immunoassay measurements of CBP and p300 levels with dCBP-30 or dCBP-1 treatment over 24 h in MM1.S cells, 10 nM. (C) Global proteomic assessment of dCBP-30 treatment (10 nM, 4 h) in MM1.S cells. (D and E) Immunoblotting results in MM1.S cells showing effects of dCBP-30, GNE-781, and A-485 on (D) histone H3 (H3K18ac and H3K27ac) and (E) histone H2B acetylation levels (H2BK5ac, H2BK20ac). (F) MM1.S cells were treated with 10 nM of either dCBP-1 or dCBP-30 over 24 h, followed by blotting for H2BK5ac and H2BK20ac. Total histone H3 or H2B levels are shown as control. See also and .

Journal: Cell reports

Article Title: An orally active dual CBP/p300 degrader targets core dependencies of multiple myeloma

doi: 10.1016/j.celrep.2026.117464

Figure Lengend Snippet: (A) Immunoassay measurements of CBP, p300, and BRD4 levels with dCBP-30 (top) or dCBP-1 (bottom) dose-response treatments with 4 h drug exposure in MM1.S cells; vinculin levels shown as loading controls. (B) Time-course immunoassay measurements of CBP and p300 levels with dCBP-30 or dCBP-1 treatment over 24 h in MM1.S cells, 10 nM. (C) Global proteomic assessment of dCBP-30 treatment (10 nM, 4 h) in MM1.S cells. (D and E) Immunoblotting results in MM1.S cells showing effects of dCBP-30, GNE-781, and A-485 on (D) histone H3 (H3K18ac and H3K27ac) and (E) histone H2B acetylation levels (H2BK5ac, H2BK20ac). (F) MM1.S cells were treated with 10 nM of either dCBP-1 or dCBP-30 over 24 h, followed by blotting for H2BK5ac and H2BK20ac. Total histone H3 or H2B levels are shown as control. See also and .

Article Snippet: GNE-781 , MedChem Express , Cat# HY-108696; CAS: 1936422-33-1.

Techniques: Western Blot, Control

(A) Clustered heatmap of A-485, GNE-781, dCBP-1, and dCBP-30 effects on the viability of a panel of 25 multiple myeloma cell lines, represented by the AUC of a nine-point dose-response ATP-based luminescence viability assay with five days of drug exposure. Clustering was performed by Euclidean distance using Morpheus ( software.broadinstitute.org/morpheus ). (B) Quantification of AUCs across cell line panel; **** p < 0.0001; * p < 0.05; line on each plot represents median. (C) Dose-response curves for each drug in four exemplary cell lines from (A): KMS-27, MM1.S, OPM-2, and NCI-H929. Data were normalized to DMSO-treated control cells; error bars represent ± SD of two replicates. (D) Growth-over-time in MM1.S cells comparing 10 nM and 100 nM of dCBP-1 and dCBP-30 (left) and dCBP-30 with the inhibitors A-485 and GNE-781 (right), normalized to DMSO-treated controls. Error bars represent ± SD of three replicates. (E) Immunoblotting of cleaved PARP (cPARP) in MM1.S and OPM2 cell lines following 10 nM dCBP-30 treatment. (F) Immunoblotting of cPARP in MM1.S cells comparing dCBP-30 with GNE-781 and A-485 (48 h). (G) Washout experiments in MM1.S cells comparing apoptosis induction by dCBP-30 (10 nM) versus A-485 (1 μM). Error bars represent ± SD of two replicates. (H) Immunoblotting of c-MYC and IRF4 following 10 nM dCBP-1 or dCBP-30 in MM1.S cells. (I) Immunoblotting of c-MYC and IRF4 comparing dCBP-30 with GNE-781 and A-485, 24 h. See also .

Journal: Cell reports

Article Title: An orally active dual CBP/p300 degrader targets core dependencies of multiple myeloma

doi: 10.1016/j.celrep.2026.117464

Figure Lengend Snippet: (A) Clustered heatmap of A-485, GNE-781, dCBP-1, and dCBP-30 effects on the viability of a panel of 25 multiple myeloma cell lines, represented by the AUC of a nine-point dose-response ATP-based luminescence viability assay with five days of drug exposure. Clustering was performed by Euclidean distance using Morpheus ( software.broadinstitute.org/morpheus ). (B) Quantification of AUCs across cell line panel; **** p < 0.0001; * p < 0.05; line on each plot represents median. (C) Dose-response curves for each drug in four exemplary cell lines from (A): KMS-27, MM1.S, OPM-2, and NCI-H929. Data were normalized to DMSO-treated control cells; error bars represent ± SD of two replicates. (D) Growth-over-time in MM1.S cells comparing 10 nM and 100 nM of dCBP-1 and dCBP-30 (left) and dCBP-30 with the inhibitors A-485 and GNE-781 (right), normalized to DMSO-treated controls. Error bars represent ± SD of three replicates. (E) Immunoblotting of cleaved PARP (cPARP) in MM1.S and OPM2 cell lines following 10 nM dCBP-30 treatment. (F) Immunoblotting of cPARP in MM1.S cells comparing dCBP-30 with GNE-781 and A-485 (48 h). (G) Washout experiments in MM1.S cells comparing apoptosis induction by dCBP-30 (10 nM) versus A-485 (1 μM). Error bars represent ± SD of two replicates. (H) Immunoblotting of c-MYC and IRF4 following 10 nM dCBP-1 or dCBP-30 in MM1.S cells. (I) Immunoblotting of c-MYC and IRF4 comparing dCBP-30 with GNE-781 and A-485, 24 h. See also .

Article Snippet: GNE-781 , MedChem Express , Cat# HY-108696; CAS: 1936422-33-1.

Techniques: Viability Assay, Software, Control, Western Blot

Chemical inhibitors used in this study.

Journal: PLOS Pathogens

Article Title: Characterization of molecular mechanisms driving Merkel cell polyomavirus oncogene transcription and tumorigenic potential

doi: 10.1371/journal.ppat.1011598

Figure Lengend Snippet: Chemical inhibitors used in this study.

Article Snippet: GNE-781 , Selleckchem S8665.

Techniques: