Santa Cruz Biotechnology cdk1 2
Cdk1 2, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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kinase 1 2 cdk1 2 (Santa Cruz Biotechnology)

Santa Cruz Biotechnology kinase 1 2 cdk1 2

Antibody antigens, final dilutions, and sources used for immunohistochemical staining of baboon adrenal tissue

Kinase 1 2 Cdk1 2, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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anti-ctip (thr847) antibody (Antibodies Inc)

Antibodies Inc anti-ctip (thr847) antibody

Anti Ctip (Thr847) Antibody, supplied by Antibodies Inc, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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cdk12 (Cusabio)

Cusabio cdk12

Cdk12, supplied by Cusabio, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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cdk12 (Cell Signaling Technology Inc)

Cell Signaling Technology Inc cdk12

Selective CDK7 inhibition with YKL-5-124 leads to aberrant cell cycle progression in NB cells. (A) Analysis of target engagement in NB cells following THZ1 or YKL-5-124 treatment. Cells were treated with THZ1, YKL-5-124 or DMSO for 6 h at the indicated doses and cell lysates were incubated with 1 μM of biotinylated THZ1 (bio-THZ1) overnight. Western blot (WB) analysis of CDK7 and <t>CDK12</t> in the immunoprecipitate (PD). (B) Dose-response curves for NB cells treated with increasing concentrations of YKL-5-124 or THZ1 for 72 h. Cytotoxicity is reported as percent cell viability relative to DMSO-treated cells. Data represent mean ± SD; n = 3. (C) Flow cytometry analysis of EdU staining in NB cells treated with 100 nM THZ1, 100 nM YKL-5-124 or DMSO for 24 h (left). The percentages of living cells in each phase of the cell cycle are shown. Quantification of staining (right), data represents mean ± SD; n = 3. (D) WB analysis of pCDK1 (Thr161), pCDK2 (Thr160) and total CDK1/2 in NB cells treated with YKL-5-124 or THZ1 at indicated doses for 6 h.

Cdk12, supplied by Cell Signaling Technology Inc, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/cdk+1+2+sc+53219/CDK12+Antibody/pmc08859926-70-48-49
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cdk9 (Santa Cruz Biotechnology)

Santa Cruz Biotechnology cdk9

Cdk9, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 94/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/cdk+1+2+sc+53219/Cdk9+Antibody/pmc12557382-270-12-13
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cdk8 (Santa Cruz Biotechnology)

Santa Cruz Biotechnology cdk8

Cdk8, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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bcl xl (Santa Cruz Biotechnology)

Santa Cruz Biotechnology bcl xl

Bcl Xl, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 96/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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cdk11 (ABclonal Biotechnology)

ABclonal Biotechnology cdk11

Cdk11, supplied by ABclonal Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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cdk6 sc 7961 (Santa Cruz Biotechnology)

Santa Cruz Biotechnology cdk6 sc 7961

Cdk6 Sc 7961, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 97/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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ctip (Santa Cruz Biotechnology)

Santa Cruz Biotechnology ctip

RB regulated CDK2-mediated <t>CtIP</t> phosphorylation <t>on</t> <t>Thr847.</t> ( A ): RB was knocked down in cells treated with 150nM CPT. Actin was used as the loading control ( B ): Equal expression levels of CtIP were found in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control ( C ): A lack of phosphorylation on CtIP T847 was observed in RB knocked-down cells treated with 150nM CPT for 24 h. Actin was used as the loading control ( D ): Less phosphorylation on CtIP T847 was observed in U2OS cells treated with 15 μM CDK2 inhibitor, roscovitine, and 150nM CPT for 24 h. GAPDH was used as the loading control. ( E ): Equal expression level of CDK1/2 in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control. ( F ): CtIP was knocked down in cells treated with 150nM CPT. Tubulin was used as the loading control. ( G ): A lack of phosphorylation on CtIP Thr847 was detected in CtIP knocked-down cells treated with 150nM CPT for 24 h. An equal expression level of CDK1/2 was detected in CtIP knocked-down cells and control treated cells. Tubulin was used as the loading control.

Ctip, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/cdk+1+2+sc+53219/CtIP+Antibody/pmc07730402-200-15-16
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cdk4 (Cell Signaling Technology Inc)

Cell Signaling Technology Inc cdk4

Cdk4, supplied by Cell Signaling Technology Inc, used in various techniques. Bioz Stars score: 96/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Image Search Results

Journal: GeroScience

Article Title: Female baboon adrenal zona fasciculata and zona reticularis regulatory and functional proteins decrease across the life course

doi: 10.1007/s11357-024-01080-9

Figure Lengend Snippet: Antibody antigens, final dilutions, and sources used for immunohistochemical staining of baboon adrenal tissue

Article Snippet: Table 2 Antibody Company Cat # Concentration Negative control Data sheet Citrate synthase (CS) Santa Cruz sc-390693 1:150 Mouse IgG cell sc-390693 (scbt.com) Steroidogenic acute regulatory protein (StAR) Santa Cruz sc-166821 1:2000 Mouse IgG cell sc-166821 (scbt.com) Mechanistic target of rapamycin (mTOR) Santa Cruz sc-517464 1:50 Mouse IgG cell SCBT Cyclin-dependent kinase 4 (CdK4) Santa Cruz sc-166373 1:100 Mouse IgG cell sc-166373 (scbt.com) Cyclin-dependent kinase 1/2 (CdK1,2) Santa Cruz sc-53219 1:50 Mouse IgG cell sc-53219 (scbt.com) Cyclophilin D (CPY40) abcam ab181983 1:500 Normal rabbit serum datasheet_181983 (2).pdf Protein Ki67 (Ki67) Novocastra NCL-ki67-mm1 1:50 Mouse IgG cell Novocastra Ki67 Antibody for IHC Staining (leicabiosystems.com) Nitrotyrosine (NT) Santa Cruz sc-32757 1:500 Mouse IgG cell sc-32757 (scbt.com) Glucocorticoid receptor (GR) Santa Cruz sc-393232 1:50 Mouse IgG cell sc-393232.qxp (scbt.com) Cyclin-dependent kinase inhibitor 1 (P21) Santa Cruz sc-817 1:150 Mouse IgG cell sc-817 (scbt.com) Proliferating cell nuclear antigen (PCNA) Santa Cruz sc-56 1:1000 Mouse IgG cell sc-56 (scbt.com) ATP-synthase (ATP5A) Santa Cruz sc- 136,178 1:200 Mouse IgG cell sc-136178 (scbt.com) Open in a separate window Antibody antigens, final dilutions, and sources used for immunohistochemical staining of baboon adrenal tissue.

Techniques: Immunohistochemical staining, Staining, Concentration Assay, Negative Control, Immunohistochemistry

Immunostaining in the ZF for all 12 proteins at the extremes of the age range—a young age of 8.9 years and an old age of 21.3 years. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Journal: GeroScience

Article Title: Female baboon adrenal zona fasciculata and zona reticularis regulatory and functional proteins decrease across the life course

doi: 10.1007/s11357-024-01080-9

Figure Lengend Snippet: Immunostaining in the ZF for all 12 proteins at the extremes of the age range—a young age of 8.9 years and an old age of 21.3 years. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Techniques: Immunostaining

Immunostaining in the ZR for all 12 proteins at the extremes of the age range—a young age of 8.9 years and an old age of 21.3 years. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Journal: GeroScience

Article Title: Female baboon adrenal zona fasciculata and zona reticularis regulatory and functional proteins decrease across the life course

doi: 10.1007/s11357-024-01080-9

Figure Lengend Snippet: Immunostaining in the ZR for all 12 proteins at the extremes of the age range—a young age of 8.9 years and an old age of 21.3 years. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Techniques: Immunostaining

Percentage annual change in area of tissue stained for all 12 proteins in the adrenal ZF (blue) and ZR (red) of 28 female baboons. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Journal: GeroScience

Article Title: Female baboon adrenal zona fasciculata and zona reticularis regulatory and functional proteins decrease across the life course

doi: 10.1007/s11357-024-01080-9

Figure Lengend Snippet: Percentage annual change in area of tissue stained for all 12 proteins in the adrenal ZF (blue) and ZR (red) of 28 female baboons. Abbreviations: mechanistic target of rapamycin (mTOR); cyclin-dependent kinase 4 (CDK4); cyclin-dependent kinase 1/2 (CDK1,2); protein Ki67 (Ki67); proliferating cell nuclear antigen (PCNA); cyclin-dependent kinase inhibitor 1 (P21); steroidogenic acute regulatory protein (StAR); glucocorticoid receptor (GR); citrate synthase (CS); cyclophilin D (CPY40); ATP-synthase (ATP5A); nitrotyrosine (NT)

Techniques: Staining

Yearly percentage change in staining (% area of tissue stained) for each of the 12 proteins in the ZF and ZR

Journal: GeroScience

Article Title: Female baboon adrenal zona fasciculata and zona reticularis regulatory and functional proteins decrease across the life course

doi: 10.1007/s11357-024-01080-9

Figure Lengend Snippet: Yearly percentage change in staining (% area of tissue stained) for each of the 12 proteins in the ZF and ZR

Techniques: Staining

Journal: Frontiers in Oncology

Article Title: Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma

doi: 10.3389/fonc.2021.773186

Figure Lengend Snippet: Selective CDK7 inhibition with YKL-5-124 leads to aberrant cell cycle progression in NB cells. (A) Analysis of target engagement in NB cells following THZ1 or YKL-5-124 treatment. Cells were treated with THZ1, YKL-5-124 or DMSO for 6 h at the indicated doses and cell lysates were incubated with 1 μM of biotinylated THZ1 (bio-THZ1) overnight. Western blot (WB) analysis of CDK7 and CDK12 in the immunoprecipitate (PD). (B) Dose-response curves for NB cells treated with increasing concentrations of YKL-5-124 or THZ1 for 72 h. Cytotoxicity is reported as percent cell viability relative to DMSO-treated cells. Data represent mean ± SD; n = 3. (C) Flow cytometry analysis of EdU staining in NB cells treated with 100 nM THZ1, 100 nM YKL-5-124 or DMSO for 24 h (left). The percentages of living cells in each phase of the cell cycle are shown. Quantification of staining (right), data represents mean ± SD; n = 3. (D) WB analysis of pCDK1 (Thr161), pCDK2 (Thr160) and total CDK1/2 in NB cells treated with YKL-5-124 or THZ1 at indicated doses for 6 h.

Article Snippet: The following antibodies were used: Pol II CTD S2 (Bethyl cat# A300-654A, 1:10,000); Pol II CTD S5 (Bethyl cat# A300-655A, 1:10,000); Pol II (Santa Cruz cat# sc-899, 1:1000); cleaved PARP (Cell Signaling cat# 9541, 1:1000); Cleaved Caspase-3 (Cell Signaling cat# 9661, 1:1000); GAPDH (Cell Signaling cat# 2118S, 1:4000); CDK12 (Cell Signaling cat# 11973S, 1:1000); CDK7 (Santa Cruz cat# sc-365075, 1: 1000); MYCN (Cell Signaling cat# 9405S, 1: 1000); CDK1 (Santa Cruz cat# sc-53219, 1:1000), pCDK1 (Cell Signaling cat# 9114, 1:1000); CDK2 (Cell Signaling cat#2546, 1:1000), pCDK2 (Cell Signaling cat# 2561, 1:1000); cyclin H (Santa Cruz #sc-609, m1:1000).

Techniques: Inhibition, Drug discovery, Incubation, Western Blot, Flow Cytometry, Staining

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Representative CDK9 inhibitors.

Article Snippet: Various primary antibodies were used to detect CDK9 (Cell Signaling Technology, 2316), CDK9 (Santa Cruz, sc-13130), ACTIN (Proteintech, 66009-1-Ig), GAPDH (Cell Signaling Technology, 2118), CDK1/2 (Santa Cruz, sc-53219), CDK4 (Cell Signaling Technology, 12790), CDK5 (Santa Cruz, sc-173), CDK6 (Cell Signaling Technology, 13331), CDK7 (Bethyl Laboratories, A300-405A), CDK8 (Santa Cruz, sc-13155), CDK11 (Abclonal, A12830), CDK12 (Cusabio, CSB-PA882147LA01HU), cleaved caspase-3 (Diagbio, db15982), cleaved PARP (Cell Signaling Technology, 5625), BCL-xL (Santa Cruz, sc-8392), E2F1 (Cell Signaling Technology, 3742), IKZF1 (Genetex, GTX124438), IKZF3 (Cell Signaling Technology, 15103), MCL1 (Diagbio, db11616), MYC (Cell Signaling Technology, 5605), RNA polymerase II Rpb1 (Cell Signaling Technology, 14958), and phospho-Rpb1 CTD Ser2 (Cell Signaling Technology, 13499).

Techniques:

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Representative CDK9 degraders.

Techniques:

Design of the CDK9 degrader. (A) Docking model of CDK9 inhibitor SNS032 to CDK9 enzyme (PDB code 8K5R ). (B) Docking model of CRBN ligand TX-16 to DDB1-CRBN E3 ubiquitin ligase (PDB code 4CI2 ). (C) Structures of the CDK9 inhibitor, degrader, and CRBN ligand.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Design of the CDK9 degrader. (A) Docking model of CDK9 inhibitor SNS032 to CDK9 enzyme (PDB code 8K5R ). (B) Docking model of CRBN ligand TX-16 to DDB1-CRBN E3 ubiquitin ligase (PDB code 4CI2 ). (C) Structures of the CDK9 inhibitor, degrader, and CRBN ligand.

Techniques: Ubiquitin Proteomics

Temporal effect and mechanistic investigation of 14 (dCDK9-202) on CDK9 degradation. (A) CDK9 protein levels in TC-71 cells upon time-course treatment with dCDK9-202 (10 nM). (B) Mechanistic investigation of CDK9 degradation induced by dCDK9-202 in the TC-71 cell line. Cells were pretreated 2 h with CDK9 inhibitor 6 (SNS032, 10 μM), thalidomide (10 μM), (R)-MG132 (5 μM), and MLN4924 (2 μM) followed by 4 h treatment with dCDK9-202 at 20 nM concentration.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Temporal effect and mechanistic investigation of 14 (dCDK9-202) on CDK9 degradation. (A) CDK9 protein levels in TC-71 cells upon time-course treatment with dCDK9-202 (10 nM). (B) Mechanistic investigation of CDK9 degradation induced by dCDK9-202 in the TC-71 cell line. Cells were pretreated 2 h with CDK9 inhibitor 6 (SNS032, 10 μM), thalidomide (10 μM), (R)-MG132 (5 μM), and MLN4924 (2 μM) followed by 4 h treatment with dCDK9-202 at 20 nM concentration.

Techniques: Concentration Assay

Degradation of CDK9 by 13 and 14 (dCDK9-202) across multiple cell lines. (A–D) Examination of dose-dependent CDK9 degradation by 13 and 14 (dCDK9-202) in TC-71, U87, SKUT1, and RH5. Cells were treated with increasing concentrations of indicated compounds for 6 h. (E) Effects of 22 on CDK9 protein. TC-71 cells were treated with the indicated concentration of 22 for 6 h.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Degradation of CDK9 by 13 and 14 (dCDK9-202) across multiple cell lines. (A–D) Examination of dose-dependent CDK9 degradation by 13 and 14 (dCDK9-202) in TC-71, U87, SKUT1, and RH5. Cells were treated with increasing concentrations of indicated compounds for 6 h. (E) Effects of 22 on CDK9 protein. TC-71 cells were treated with the indicated concentration of 22 for 6 h.

Techniques: Concentration Assay

Antiproliferative activities of CDK9 degraders 13 and 14 (dCDK9-202) against multiple cancer cell lines. (A) Effect of dCDK9-202 treatment (50 nM, 24 h) on BrdU incorporation by TC-71 cells. Data are presented as mean ± SEM; **, p < 0.01 based on two-tailed t test. (B) Effect of dCDK9-202 treatment (50 nM, 24 h) on caspase-3/7 activity in TC-71 cells. Data are presented as mean ± SEM; ***, p < 0.001 based on two-tailed t test. (C) Effect of dCDK9-202 treatment (24 h) on intracellular levels of CDK9 and apoptotic markers in TC-71 cells. (D) Effect of 13 and 14 (dCDK9-202) treatment on cellular viabilities of indicated cancer cell lines. IC 50 is presented as mean ± SEM with three independent replicates.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Antiproliferative activities of CDK9 degraders 13 and 14 (dCDK9-202) against multiple cancer cell lines. (A) Effect of dCDK9-202 treatment (50 nM, 24 h) on BrdU incorporation by TC-71 cells. Data are presented as mean ± SEM; **, p < 0.01 based on two-tailed t test. (B) Effect of dCDK9-202 treatment (50 nM, 24 h) on caspase-3/7 activity in TC-71 cells. Data are presented as mean ± SEM; ***, p < 0.001 based on two-tailed t test. (C) Effect of dCDK9-202 treatment (24 h) on intracellular levels of CDK9 and apoptotic markers in TC-71 cells. (D) Effect of 13 and 14 (dCDK9-202) treatment on cellular viabilities of indicated cancer cell lines. IC 50 is presented as mean ± SEM with three independent replicates.

Techniques: BrdU Incorporation Assay, Two Tailed Test, Activity Assay

Compound 14 (dCDK9-202) selectively proteolyzes CDK9 to impair Pol2 function and cancer-addicted transcriptome. (A) Temporal effect of dCDK9-202 treatment on CDK and IKZF proteins in TC-71 cells. (B, C) Effect of 14 (dCDK9-202) and 6 (SNS032) treatment on Rpb1, phosphorylation of Rpb1 CTD ser2 , and key targets in downstream signaling pathways. (D, E) RNA-seq analysis of TC-71 cells upon dCDK9-202 (10 nM, 8 h) and SNS032 (10 nM, 8 h) treatments. (F) GSEA showing representative biological pathways affected by dCDK9-202 treatment in TC-71.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Compound 14 (dCDK9-202) selectively proteolyzes CDK9 to impair Pol2 function and cancer-addicted transcriptome. (A) Temporal effect of dCDK9-202 treatment on CDK and IKZF proteins in TC-71 cells. (B, C) Effect of 14 (dCDK9-202) and 6 (SNS032) treatment on Rpb1, phosphorylation of Rpb1 CTD ser2 , and key targets in downstream signaling pathways. (D, E) RNA-seq analysis of TC-71 cells upon dCDK9-202 (10 nM, 8 h) and SNS032 (10 nM, 8 h) treatments. (F) GSEA showing representative biological pathways affected by dCDK9-202 treatment in TC-71.

Techniques: Phospho-proteomics, Protein-Protein interactions, RNA Sequencing

Pharmacodynamic analysis of 14 (dCDK9-202) in the TC-71 xenograft model. (A) In vivo PK of compound 14 in mice. (B) Western blotting analysis of CDK9 protein in the TC-71 xenograft lysate. Immunocompromised mice bearing subcutaneous TC-71 tumors were treated with a single IV administration of 14 (dCDK9-202) at a dose of 10 mg/kg. Mice were euthanized at indicated time points for collection of tumor tissues for analysis. (C) Western blotting analysis of CDK9 protein in the spleens of mice receiving a single IV administration of 14 (dCDK9-202) at 10 mg/kg.

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Pharmacodynamic analysis of 14 (dCDK9-202) in the TC-71 xenograft model. (A) In vivo PK of compound 14 in mice. (B) Western blotting analysis of CDK9 protein in the TC-71 xenograft lysate. Immunocompromised mice bearing subcutaneous TC-71 tumors were treated with a single IV administration of 14 (dCDK9-202) at a dose of 10 mg/kg. Mice were euthanized at indicated time points for collection of tumor tissues for analysis. (C) Western blotting analysis of CDK9 protein in the spleens of mice receiving a single IV administration of 14 (dCDK9-202) at 10 mg/kg.

Techniques: In Vivo, Western Blot

Antitumor activity of 14 (dCDK9-202) in the TC-71 xenograft model in immunocompromised mice. (A) Changes in tumor volume during dCDK9-202, 6 (SNS032), or 10 (THAL-SNS032) treatments (10 mg/kg, i.v., qod). (B) Tumor weight at the end point of experiment. (C) Image of subcutaneous TC-71 xenograft tumors harvested at the end point of experiment. (D) Body weight of recipient mice during treatments. (E) Western blot analysis of CDK9 protein levels in tumor lysates harvested 4 h after final treatment (representative samples shown). Data in panels A, B, and D are presented as mean ± SD and were analyzed by one-way ANOVA (significance denoted as n.s., not significant; *, p < 0.05; **, p < 0.01; ***, p < 0.001).

Journal: Journal of Medicinal Chemistry

Article Title: Discovery of dCDK9-202 as a Highly Potent and Selective PROTAC CDK9 Degrader with Strong In Vivo Antitumor Activity

doi: 10.1021/acs.jmedchem.5c01111

Figure Lengend Snippet: Antitumor activity of 14 (dCDK9-202) in the TC-71 xenograft model in immunocompromised mice. (A) Changes in tumor volume during dCDK9-202, 6 (SNS032), or 10 (THAL-SNS032) treatments (10 mg/kg, i.v., qod). (B) Tumor weight at the end point of experiment. (C) Image of subcutaneous TC-71 xenograft tumors harvested at the end point of experiment. (D) Body weight of recipient mice during treatments. (E) Western blot analysis of CDK9 protein levels in tumor lysates harvested 4 h after final treatment (representative samples shown). Data in panels A, B, and D are presented as mean ± SD and were analyzed by one-way ANOVA (significance denoted as n.s., not significant; *, p < 0.05; **, p < 0.01; ***, p < 0.001).

Techniques: Activity Assay, Western Blot

RB regulated CDK2-mediated CtIP phosphorylation on Thr847. ( A ): RB was knocked down in cells treated with 150nM CPT. Actin was used as the loading control ( B ): Equal expression levels of CtIP were found in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control ( C ): A lack of phosphorylation on CtIP T847 was observed in RB knocked-down cells treated with 150nM CPT for 24 h. Actin was used as the loading control ( D ): Less phosphorylation on CtIP T847 was observed in U2OS cells treated with 15 μM CDK2 inhibitor, roscovitine, and 150nM CPT for 24 h. GAPDH was used as the loading control. ( E ): Equal expression level of CDK1/2 in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control. ( F ): CtIP was knocked down in cells treated with 150nM CPT. Tubulin was used as the loading control. ( G ): A lack of phosphorylation on CtIP Thr847 was detected in CtIP knocked-down cells treated with 150nM CPT for 24 h. An equal expression level of CDK1/2 was detected in CtIP knocked-down cells and control treated cells. Tubulin was used as the loading control.

Journal: International Journal of Molecular Sciences

Article Title: RB Regulates DNA Double Strand Break Repair Pathway Choice by Mediating CtIP Dependent End Resection

doi: 10.3390/ijms21239176

Figure Lengend Snippet: RB regulated CDK2-mediated CtIP phosphorylation on Thr847. ( A ): RB was knocked down in cells treated with 150nM CPT. Actin was used as the loading control ( B ): Equal expression levels of CtIP were found in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control ( C ): A lack of phosphorylation on CtIP T847 was observed in RB knocked-down cells treated with 150nM CPT for 24 h. Actin was used as the loading control ( D ): Less phosphorylation on CtIP T847 was observed in U2OS cells treated with 15 μM CDK2 inhibitor, roscovitine, and 150nM CPT for 24 h. GAPDH was used as the loading control. ( E ): Equal expression level of CDK1/2 in both RB knocked-down cells and control treated cells treated with 150nM CPT for 24 h. Tubulin was used as the loading control. ( F ): CtIP was knocked down in cells treated with 150nM CPT. Tubulin was used as the loading control. ( G ): A lack of phosphorylation on CtIP Thr847 was detected in CtIP knocked-down cells treated with 150nM CPT for 24 h. An equal expression level of CDK1/2 was detected in CtIP knocked-down cells and control treated cells. Tubulin was used as the loading control.

Article Snippet: The membranes were probed with primary antibodies against RB (Abcam, Cambridge, United Kingdom, ab181616, 1:500), CtIP (Santa Cruz, Dallas, TX, USA, sc-271339, 1:500), phospho-Thr847 CtIP (PhosphoSolutions, Aurora, CO, USA, p1012-847, 1:500), and CDK1/2 (Santa Cruz USA, sc-53219, 1:200), followed by incubation with the appropriate secondary antibodies coupled with horseradish peroxidase.

Techniques: Phospho-proteomics, Control, Expressing

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