| Identification | Back Directory | [Name]
3-Pyridinecarboxamide, 1,6-dihydro-1,5-dimethyl-N-[(1R)-2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]-6-oxo-N-[(2S)-2-phenyl-2-(2-pyridinyl)ethyl]- | [CAS]
2752331-09-0 | [Synonyms]
3-Pyridinecarboxamide, 1,6-dihydro-1,5-dimethyl-N-[(1R)-2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]-6-oxo-N-[(2S)-2-phenyl-2-(2-pyridinyl)ethyl]- | [Molecular Formula]
C29H34N4O4 | [MOL File]
2752331-09-0.mol | [Molecular Weight]
502.6 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
BD2: 8.3 (pIC50) | [References]
[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. DOI:10.1021/acs.jmedchem.1c00412 |
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