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PBRM1 bromodomains

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163410
    AU-24118
    1 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
    AU-24118
  • HY-151538
    PBRM1-BD2-IN-8

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity .
    PBRM1-BD2-IN-8
  • HY-151532
    PBRM1-BD2-IN-5

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer .
    PBRM1-BD2-IN-5
  • HY-149026
    GNE-064

    		Epigenetic Reader Domain Others
    GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis .
    GNE-064
  • HY-150289
    GNE-235

    		Epigenetic Reader Domain Cancer
    GNE-235 is a compound selective for the second bromodomain of PBRM1, with a KD of 0.28 ± 0.02 μM. GNE-235 can be used for evaluation of the cellular function of PBRM1 .
    GNE-235
  • HY-151531
    PBRM1-BD2-IN-4

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 Bromodomain inhibitor with Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer .
    PBRM1-BD2-IN-4
  • HY-151528
    PBRM1-BD2-IN-1

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer .
    PBRM1-BD2-IN-1
  • HY-161881
    SMARCA2-IN-9

    		Epigenetic Reader Domain Cancer
    SMARCA2-IN-9 (compound 11) is a SMARCA2, PBRM1 bromodomains 2 (PBRM1(2)), and PBRM1 bromodomains 5 (PBRM1(5)) inhibitor with Kd values of 1.6 μM, 2.5 μM, and 3.95 μM, respectively .
    SMARCA2-IN-9
  • HY-151533
    PBRM1-BD2-IN-6

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 μM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer .
    PBRM1-BD2-IN-6
  • HY-151529
    PBRM1-BD2-IN-2

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer .
    PBRM1-BD2-IN-2
  • HY-171774
    PBRM1/SMARCA2,4-ligand-1

    		Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a Ligand for Target Protein for PROTAC that binds to PBRM1, SMARCA2, and SMARCA4. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410) .
    PBRM1/SMARCA2,4-ligand-1
  • HY-151534
    PBRM1-BD2-IN-7

    		Epigenetic Reader Domain Cancer
    PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer .
    PBRM1-BD2-IN-7

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