GSK 525762A
| CAS No. | 1260907-17-2 | Cat. No. | BCP07337 |
| Name | GSK 525762A | ||
| Synonyms | GSK525762A;GSK-525762A;I-BET762;I-BET 762; | ||
| Formula | C22H22ClN5O2 | M. Wt | 423.9 |
| Description | I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes. I-BET-762 treatment during the first 2 d of differentiation alters CD4+ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines. | ||
| Pathways | Epigenetics | ||
| Targets | Epigenetic Reader Domain | ||
Structure
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