| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 83.33 mg/mL (201.05 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.96 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | immuno-inflammation | GSK-046 | GSK046 | GSK 046 | EpigeneticReaderDomain | Epigenetic Reader Domain | BRDT-BD2 | BRDT | BRD4-BD2 | BRD4 | BRD3-BD2 | BRD3 | BRD2-BD2 | BRD2 | BD2 |
| Inhibitors Related | ABBV-744 | SNDX-5613 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Curcumin | dBET6 | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Histone Modification Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | PPI Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library |