Potent SMARCA2/4 inhibitor
FHT 2344 is a potent allosteric and ATP-competitive inhibitor of SMARCA2/SMARCA4 ATPases (also known as BRM/BRG1) of the BAF complex (IC50 values are 13.8 and 26.1 nM at SMARCA2 and SMARCA4, respectively). FHT 2344 inhibits SMARCA2 transcriptional activity in a BRG1-mutant cell line and SMARCA4 transcription in a BRM-mutant cell line (IC50 values are 29.8 and 30.2 nM, respectively). Dose-dependently reduces tumor growth in a uveal melanoma xenograft model and suppresses SOX10 transcription.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151425 |
| Réf. fabricant | 30000026 |
| Nom chimique ou matériau | N-[(1S)-1-(Methoxymethyl)-2-[[4-[3-(1-methyl-1H-pyrazol-3-yl)phenyl]-2-thiazolyl]amino]-2-oxoethyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide |
| CAS | 2468058-90-2 |
| Quantité | 10 mg |
| Cible | Bromodomain Inhibitors |
| Formule moléculaire | C<sub>23</sub>H<sub>24</sub>N<sub>6</sub>O<sub>5</sub>S<sub>2</sub> |
| Pureté | 0.95 |
