Potent and selective SMARCA4/2 inhibitor
FHT 1015 is a potent and selective allosteric inhibitor of SMARCA4/SMARCA2 ATPase (also known as BRG1/BRM respectively) of the BAF (BRG/Brahma-associated factors) complex, with IC50s of ≤ 10 nM. Exhibits selectivity for SMARCA4/SMARCA2 over related CHD4 (IC50 of > 400 μM). Mutations in I1143 on SMARCA4 and I1173 on SMARCA2 render these proteins resistant to inhibition by FHT 1015. The compound induces lineage-specific changes in chromatin accessibility in different cancer cell lines, preventing binding of cancer-associated transcription factors, SOX10 and MITF transcription factors.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151168 |
| Réf. fabricant | 30000014 |
| Nom chimique ou matériau | (S)-1-(Methylsulfonyl)-N-[4-(methylthio)-1-oxo-1-[[4-[3-(pyridin-4-yl)phenyl]thiazol-2-yl]amino]butan-2-yl]-1H-pyrrole-3-carboxamide |
| CAS | 2368903-18-6 |
| Quantité | 2 mg |
| Cible | Bromodomain Inhibitors |
| Formule moléculaire | C<sub>25</sub>H<sub>25</sub>N<sub>5</sub>O<sub>4</sub>S<sub>3</sub> |
| Pureté | 0.95 |
