GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 2 mg | In stock | $ 82 | |
| 4 mg | In stock | $ 147 | |
| 8 mg | In stock | $ 248 | |
| 20 mg | In stock | $ 460 | |
| 40 mg | In stock | $ 736 |
| Description | GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain. |
| Targets&IC50 | BRPF1:8.1(pIC50) |
| 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. |
| 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. |
| CAS No. | 1910124-24-1 |
| Chemical Formula | C22H27N5O3 |
| Molecular Weight | 409.49 |
| Solubility | Ethanol: 81 mg/mL (197.81 mM) DMSO: 29 mg/mL |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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