GSK046 | BET BD2 inhibitor | Probechem Biochemicals

Chemical Structure : GSK046

CAS No.: 2474876-09-8

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GSK046 (GSK-046, iBET-BD2)

货号: PC-72182Not For Human Use, Lab Use Only.

GSK046 (GSK-046, iBET-BD2) is a potent, highly selective inhibitor of BET BD2 with pIC50 of 7.3 (BRD4 BD2), >1000-fold over BRD4 BD1.

规格	价格	库存
5 mg	￥1780	In stock
10 mg	￥2780	In stock
25 mg	￥4580	In stock
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100 mg		Get quote

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生物&药学活性

GSK046 (GSK-046, iBET-BD2) is a potent, highly selective inhibitor of BET BD2 with pIC50 of 7.3 (BRD4 BD2), >1000-fold over BRD4 BD1.
GSK046 (iBET-BD2) potently inhibits BRD2/BRD3/BRDT BD2 with pIC50 of 6.6/7.0/6.7.
GSK046 (iBET-BD2) inhibits MCP-1 cytokine release (pIC50=7.5) with a minimal drop-off from the biochemical BRD4 BD2 potency observed in an LPS-stimulated PBMC cellular assay.
GSK046 (iBET-BD2) is efficacious in a broad range of inflammatory pathologies and selective BD2 inhibition may be a useful new therapeutic strategy for immunoinflammatory diseases.

物理化学性质&存储条件

分子量	414.477
分子式	C23H27FN2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO (4.1 mg/mL)
Chemical Name/SMILES	4-Acetamido-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-((S)-1-phenylethoxy)benzamide

参考文献

1. Preston A, et al. J Med Chem. 2020 Sep 10;63(17):9070-9092.

2. Seal JT, et al. J Med Chem. 2020 Sep 10;63(17):9093-9126.

GSK046 (GSK-046, iBET-BD2)

生物&药学活性

物理化学性质&存储条件

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GSK046 (GSK-046, iBET-BD2)

生物&药学活性

物理化学性质&存储条件

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