| Bioactivity | GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases[1]. |
| In Vivo | GSK040 (1 mg/kg; i.v.) exhibits t1/2 (0.19 h), CLb (50 mL/min/kg) and Vss (0.6 L/kg) in rats[1].GSK040 (3 mg/kg; p.o.) exhibits oral bioavailability (16%), tmax (0.25 h), Cmax (398 nM) in rats[1]. |
| Name | GSK040 |
| CAS | 2752331-09-0 |
| Formula | C29H34N4O4 |
| Molar Mass | 502.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Rianjongdee F, et, al. Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit. J Med Chem. 2021 Jul 12. |