Name | GSK046 |
Description | GSK046 (iBET-BD2) is a potent, selective, and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50 values of 264 nM [BRD2 BD2], 98 nM [BRD3 BD2], 49 nM [BRD4 BD2], and 214 nM [BRDT BD2], respectively. It exhibits immunomodulatory activity. |
In vivo | GSK046 (40 mg/kg/QD;?s.c. for 14 days) has immunomodulatory activity.?GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg).?GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 83.33 mg/mL (201.05 mM), Sonication is recommended.
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Keywords | GSK-046 | Epigenetic Reader Domain | BRDT | BRD2 | inhibit | GSK046 | immuno-inflammation | BRD4 | GSK 046 | Inhibitor | BD2 | BRD3 |
Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
Related Compound Libraries | 细胞重编程化合物库 | 组蛋白修饰化合物库 | 经典已知活性库 | 表观遗传库 | 抑制剂库 | NO PAINS 化合物库 | 口服活性化合物库 | PPI抑制剂库 | 已知活性化合物库 |