| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [color ]
white to beige | [InChIKey]
ZORLJXWXFABTPZ-CTNGQTDRSA-N | [SMILES]
C[C@H](C1=CC=CC=C1)N2C(COC)=NC3=C2C(C=C4OC[C@@H]5CNCC5)=C(N=C3)C=C4C6=C(C)ON=C6C |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2BDR3BRD4BRDT. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferationinducing cell cycle arrest and apoptosis. | [IC 50]
BRD2 BD1: 75 nM (IC50); BRD3 BD1: 41 nM (IC50); BRD4-BD1: 41 nM (IC50); BRDT BD1: 143 nM (IC50) | [References]
[1] Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394. DOI:10.1126/science.aaz8455 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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