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brd4 protac a1874  (MedChemExpress)


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    Structured Review

    MedChemExpress brd4 protac a1874
    A) Structure of the MDM2-recruiting <t>BRD4</t> degrader <t>A1874</t> formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.
    Brd4 Protac A1874, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/brd4+protac+a1874/bio_rxiv__64898__2026__01__12__698947-168-11-15?v=MedChemExpress
    Average 94 stars, based on 2 article reviews
    brd4 protac a1874 - by Bioz Stars, 2026-08
    94/100 stars

    Images

    1) Product Images from "PROTAC-Driven Protective Therapy increases the therapeutic window of anticancer drugs"

    Article Title: PROTAC-Driven Protective Therapy increases the therapeutic window of anticancer drugs

    Journal: bioRxiv

    doi: 10.64898/2026.01.12.698947

    A) Structure of the MDM2-recruiting BRD4 degrader A1874 formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.
    Figure Legend Snippet: A) Structure of the MDM2-recruiting BRD4 degrader A1874 formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.

    Techniques Used: Western Blot, Control, Expressing, Immunofluorescence

    A) BRD4, MDM2, p53, and p21 protein levels in a panel of cancer cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. Left panel displays colon cancer lines, including TP53 WT (HCT116 and RKO) and mutant (DLD1 and HT29) cells. Middle panel displays ovarian cancer cell lines, including TP53 WT (A2780) and mutant (ES2, OVCAR8 and SKOV3) cells. Right panel displays BJ and RPE1 p53-proficient primary cell lines. B) MDM2 mRNA expression levels in the indicated cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). C) Schematic representation of the CRISPRa/dCas9-SAM system. It consists of a dead Cas9 (dCas9) fused to the transcriptional activator VP64. The gRNA targeting MDM2 promoter forms a complex with MS2 (blue) and recruits transcriptional p65 (orange) and HSF1 (red) activators. This induces MDM2 expression from the endogenous locus. D) MDM2 mRNA expression levels in SKOV3 transduced with E.V. or gRNAs targeting MDM2 promoter, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). E) BRD4, and MDM2 protein levels in empty vector (E.V.)-transduced or MDM2-overexpressing SKOV3 cell lines treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. F) MDM2 mRNA expression levels in the indicated cells treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3).
    Figure Legend Snippet: A) BRD4, MDM2, p53, and p21 protein levels in a panel of cancer cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. Left panel displays colon cancer lines, including TP53 WT (HCT116 and RKO) and mutant (DLD1 and HT29) cells. Middle panel displays ovarian cancer cell lines, including TP53 WT (A2780) and mutant (ES2, OVCAR8 and SKOV3) cells. Right panel displays BJ and RPE1 p53-proficient primary cell lines. B) MDM2 mRNA expression levels in the indicated cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). C) Schematic representation of the CRISPRa/dCas9-SAM system. It consists of a dead Cas9 (dCas9) fused to the transcriptional activator VP64. The gRNA targeting MDM2 promoter forms a complex with MS2 (blue) and recruits transcriptional p65 (orange) and HSF1 (red) activators. This induces MDM2 expression from the endogenous locus. D) MDM2 mRNA expression levels in SKOV3 transduced with E.V. or gRNAs targeting MDM2 promoter, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). E) BRD4, and MDM2 protein levels in empty vector (E.V.)-transduced or MDM2-overexpressing SKOV3 cell lines treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. F) MDM2 mRNA expression levels in the indicated cells treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3).

    Techniques Used: Western Blot, Control, Mutagenesis, Expressing, Transduction, Plasmid Preparation



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    MedChemExpress brd4 protac a1874
    A) Structure of the MDM2-recruiting <t>BRD4</t> degrader <t>A1874</t> formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.
    Brd4 Protac A1874, supplied by MedChemExpress, 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/brd4+protac+a1874/bio_rxiv__64898__2026__01__12__698947-168-11-15?v=MedChemExpress
    Average 94 stars, based on 1 article reviews
    brd4 protac a1874 - by Bioz Stars, 2026-08
    94/100 stars
      Buy from Supplier

    Image Search Results


    A) Structure of the MDM2-recruiting BRD4 degrader A1874 formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.

    Journal: bioRxiv

    Article Title: PROTAC-Driven Protective Therapy increases the therapeutic window of anticancer drugs

    doi: 10.64898/2026.01.12.698947

    Figure Lengend Snippet: A) Structure of the MDM2-recruiting BRD4 degrader A1874 formed by JQ1 (a BRD4 inhibitor) and Idasanutlin (an MDM2 antagonist). B) BRD4, MDM2, p53 and p21 protein levels in isogenic TP53 WT and KO HCT116 cells treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin (VLC) was used as loading control. C) MDM2 mRNA expression levels in TP53 WT and TP53 KO HCT116 cells treated with 1 µM A1874 for 24 h assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). D) Representative immunofluorescence images of MDM2 levels in TP53 WT and KO HCT116 cells upon treatment with vehicle or 1 µM A1874 for 24 h. Quantification of MDM2 nuclear intensity from 1600 cells is shown on the right. Statistical significance was determined with unpaired t-tests. **** = p < 0.0001.

    Article Snippet: Cells were treated with the following compounds at the indicated doses: BRD4 PROTAC A1874 (HY-114305, MedChemExpress) at 1 μM; PARP1 PROTACs SK-575 (HY-139156, MedChemExpress) at 100 nM and 180055 (HY-170620, MedChemExpress) at 1 μM; and PARP inhibitors Talazoparib (HY-16106, MedChemExpress) and Olaparib (HY-10162, MedChemExpress) at concentrations ranging from 48 μM to 0.02 μM in 3-fold dilutions.

    Techniques: Western Blot, Control, Expressing, Immunofluorescence

    A) BRD4, MDM2, p53, and p21 protein levels in a panel of cancer cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. Left panel displays colon cancer lines, including TP53 WT (HCT116 and RKO) and mutant (DLD1 and HT29) cells. Middle panel displays ovarian cancer cell lines, including TP53 WT (A2780) and mutant (ES2, OVCAR8 and SKOV3) cells. Right panel displays BJ and RPE1 p53-proficient primary cell lines. B) MDM2 mRNA expression levels in the indicated cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). C) Schematic representation of the CRISPRa/dCas9-SAM system. It consists of a dead Cas9 (dCas9) fused to the transcriptional activator VP64. The gRNA targeting MDM2 promoter forms a complex with MS2 (blue) and recruits transcriptional p65 (orange) and HSF1 (red) activators. This induces MDM2 expression from the endogenous locus. D) MDM2 mRNA expression levels in SKOV3 transduced with E.V. or gRNAs targeting MDM2 promoter, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). E) BRD4, and MDM2 protein levels in empty vector (E.V.)-transduced or MDM2-overexpressing SKOV3 cell lines treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. F) MDM2 mRNA expression levels in the indicated cells treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3).

    Journal: bioRxiv

    Article Title: PROTAC-Driven Protective Therapy increases the therapeutic window of anticancer drugs

    doi: 10.64898/2026.01.12.698947

    Figure Lengend Snippet: A) BRD4, MDM2, p53, and p21 protein levels in a panel of cancer cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. Left panel displays colon cancer lines, including TP53 WT (HCT116 and RKO) and mutant (DLD1 and HT29) cells. Middle panel displays ovarian cancer cell lines, including TP53 WT (A2780) and mutant (ES2, OVCAR8 and SKOV3) cells. Right panel displays BJ and RPE1 p53-proficient primary cell lines. B) MDM2 mRNA expression levels in the indicated cell lines treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). C) Schematic representation of the CRISPRa/dCas9-SAM system. It consists of a dead Cas9 (dCas9) fused to the transcriptional activator VP64. The gRNA targeting MDM2 promoter forms a complex with MS2 (blue) and recruits transcriptional p65 (orange) and HSF1 (red) activators. This induces MDM2 expression from the endogenous locus. D) MDM2 mRNA expression levels in SKOV3 transduced with E.V. or gRNAs targeting MDM2 promoter, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3). E) BRD4, and MDM2 protein levels in empty vector (E.V.)-transduced or MDM2-overexpressing SKOV3 cell lines treated with 1 µM A1874 for 24 h, assessed by western blot. Vinculin was used as loading control. F) MDM2 mRNA expression levels in the indicated cells treated with vehicle or 1 µM A1874 for 24 h, assessed by qPCR. Error bars indicate mean ± s.d. (n = 3).

    Article Snippet: Cells were treated with the following compounds at the indicated doses: BRD4 PROTAC A1874 (HY-114305, MedChemExpress) at 1 μM; PARP1 PROTACs SK-575 (HY-139156, MedChemExpress) at 100 nM and 180055 (HY-170620, MedChemExpress) at 1 μM; and PARP inhibitors Talazoparib (HY-16106, MedChemExpress) and Olaparib (HY-10162, MedChemExpress) at concentrations ranging from 48 μM to 0.02 μM in 3-fold dilutions.

    Techniques: Western Blot, Control, Mutagenesis, Expressing, Transduction, Plasmid Preparation