| Name | GSK6853 |
| Description | GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain. |
| In vitro | Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays[1]. |
| In vivo | In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 55 mg/mL (134.32 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.88 mM), Sonication is recommended.
Ethanol : 81 mg/mL (197.81 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | GSK-6853 | GSK6853 | GSK 6853 | EpigeneticReaderDomain | Epigenetic Reader Domain | BRPF3 | BRPF2 | BRPF1 |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Curcumin | dBET6 | ARV-825 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | Isoxazole |
| Related Compound Libraries | Highly Selective Inhibitor Library | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Chromatin Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
