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BET bromodomain inhibitor1

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-131061
    BET bromodomain inhibitor 1

    		Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
    BET bromodomain inhibitor 1
  • HY-100653
    AZD5153
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors .
    AZD5153
  • HY-W010649
    Isoxazole

    		HSP Epigenetic Reader Domain ATP-binding cassette (ABC) transporters Bacterial Fungal Antibiotic Infection Metabolic Disease Inflammation/Immunology Cancer
    Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​ .
    Isoxazole
  • HY-156814
    HPP-9

    		Hedgehog Cancer
    HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC50 of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity [1[.
    HPP-9
  • HY-15846A
    (Rac)-CPI-203

    		Epigenetic Reader Domain Cancer
    (Rac)-CPI-203 is a racemate of CPI-203 (HY-15846) (BET bromodomain inhibitor)
    (Rac)-CPI-203
  • HY-128977
    CD235

    		Epigenetic Reader Domain Cancer
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor .
    CD235
  • HY-W806047
    BRD4 Inhibitor-37

    		Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
    BRD4 Inhibitor-37

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