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BRDT BD1

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

1

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Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-136570
    GSK778
    1 Publications Verification

    iBET-BD1

    		 Epigenetic Reader Domain Apoptosis Inflammation/Immunology Cancer
    GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models .
    GSK778
  • HY-111422
    PLX51107
    3 Publications Verification

    		 Epigenetic Reader Domain Cancer
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
    PLX51107
  • HY-112610
    CF53

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .
    CF53
  • HY-138563
    GSK973

    		Epigenetic Reader Domain Cancer
    GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
    GSK973
  • HY-160558
    PLK1/BRD4-IN-3

    		Epigenetic Reader Domain Polo-like Kinase (PLK) Cancer
    PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively .
    PLK1/BRD4-IN-3
  • HY-138623
    GSK789

    		Epigenetic Reader Domain TNF Receptor Interleukin Related Inflammation/Immunology Cancer
    GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases .
    GSK789
  • HY-136794
    SB-284851-BT

    		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-136570A
    GSK778 hydrochloride

    iBET-BD1 hydrochloride

    		 Apoptosis Epigenetic Reader Domain Inflammation/Immunology Cancer
    GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively .
    GSK778 hydrochloride
  • HY-175033
    BRD4-IN-11

    		Epigenetic Reader Domain Phosphatase c-Myc Apoptosis Inflammation/Immunology
    BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis .
    BRD4-IN-11
  • HY-168628
    BET-IN-27

    		Epigenetic Reader Domain Cancer
    BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .
    BET-IN-27
  • HY-172210
    DDO-8958

    		Epigenetic Reader Domain Apoptosis Cancer
    DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity .
    DDO-8958
  • HY-149519
    BRD4 Inhibitor-28

    		Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
    BRD4 Inhibitor-28
  • HY-126325
    BY27

    		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-183248
    BRDT-IN-2

    		Epigenetic Reader Domain Cancer
    BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=10 μM) with higher affinity for BRDT-BD1 than BRD4-BD1. BRDT-IN-2 preferentially binds BRDT-BD1 without direct interaction with BRDT-BD1’s Arg54 residue. BRDT-IN-2 binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma .
    BRDT-IN-2
  • HY-183247
    BRDT-IN-1

    		Epigenetic Reader Domain Cancer
    BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma .
    BRDT-IN-1
  • HY-182362
    TK-285

    		Epigenetic Reader Domain Inflammation/Immunology
    TK-285 is a potent TSLP inhibitor that suppresses the production of TSLP and inhibits the expression of interleukin-33 mRNA. TK-285 exhibits a selective binding preference for the BD1 domains of BRD2, BRD3, BRD4 and BRDT. TK-285 can be used in research related to atopic dermatitis .
    TK-285
  • HY-182371
    BRD4 ligand 15

    		Epigenetic Reader Domain Ligands for Target Protein for PROTAC Others
    BRD4 ligand 15 (compound 5) is a BRD4 ligand and alkyne-modified chalcone derivative, which serves as a building block for the synthesis of BRD4-targeting PROTAC TKP-5 (HY-182370) .
    BRD4 ligand 15

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