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BET-IN-2

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137892

    Epigenetic Reader Domain Inflammation/Immunology
    GSK620, a chemical probe, is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
    GSK620
  • HY-102044

    Epigenetic Reader Domain Cancer
    BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
    BET-IN-2
  • HY-114228
    PROTAC BET degrader-2
    2 Publications Verification

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
    PROTAC BET degrader-2
  • HY-136794

    p38 MAPK Epigenetic Reader Domain Inflammation/Immunology Cancer
    SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .
    SB-284851-BT
  • HY-132230

    Epigenetic Reader Domain Inflammation/Immunology Cancer
    GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases .
    GSK040
  • HY-W1120221

    E3 Ligase Ligand-Linker Conjugates Others
    Lenalidomide-C3-NH2 is an E3 ligase ligand-linker conjugate that incorporates the Lenalidomide (HY-A0003) based CRBN ligand (HY-43722) and linker. Lenalidomide-C3-NH2 can be used for synthesis of PROTAC BET degrader-2 (HY-114228) .
    Lenalidomide-C3-NH2
  • HY-155680

    Epigenetic Reader Domain Inflammation/Immunology
    BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research .
    BET BD2-IN-1
  • HY-159602

    Epigenetic Reader Domain Cancer
    BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice .
    BET BD2-IN-3
  • HY-155809

    Epigenetic Reader Domain Cancer
    BET-IN-17 (compound 16) is a pan-inhibitor of BET with pIC50s of 7.8 and 7.6 for BET BD1 and BET BD2, respectively .
    BET-IN-17
  • HY-126325

    Epigenetic Reader Domain Cancer
    BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .
    BY27
  • HY-173315

    Epigenetic Reader Domain Cancer
    pan-BET/BD2-IN-1 (compound 6b) is a selective extra-terminal (BET) protein inhibitor (BRDT-1 Ki = 1.05 μM and BRD4-1 Ki = 0.68 μM). pan-BET/BD2-IN-1 inhibits MM.1S cancer cell growth with an IC50 of 2.6 μM .
    pan-BET/BD2-IN-1
  • HY-179588

    PROTACs Epigenetic Reader Domain c-Myc Cancer
    PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .
    PROTAC BET Degrader-14

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