High affinity and selective PCAF bromodomain inhibitor
L Moses dihydrochloride is a high affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM), which exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). L Moses exhibits >4500-fold selectivity for PCAF over BRD4. The compound inhibits Tunicamycin (Cat. No. 3516) -induced neuronal cell death by reversing the transcriptional changes associated with Tunicamycin treatment. L Moses exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC).
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-125878 |
| Réf. fabricant | 18766206 |
| Nom chimique ou matériau | (1S, 2S)-N1,N1-Dimethyl-N2-(3-methyl-1,2,4-triazolo[3,4-a]phthalazin-6-yl)-1-phenylpropane-1,2-diamine dihydrochloride |
| Plage de pourcentage du dosage | >98% |
| Quantité | 50 mg |
| Formule moléculaire | C<sub>21</sub>H<sub>24</sub>N<sub>6</sub>.2HCl |
| Poids de la formule | Observed MW: 433.38 |
