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Chemical Structure : GSK046
CAS No.: 2474876-09-8
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 414.477 | |
| Formula | C23H27FN2O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (4.1 mg/mL) |
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| Chemical Name/SMILES |
4-Acetamido-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-((S)-1-phenylethoxy)benzamide |
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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.
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