Potent and selective CDKL5 inhibitor
CAF 382 is potent and selective CDKL5 (cyclin-dependent kinase-like 5) inhibitor (IC50 = 10 nM). Exhibits nearly 100-fold selectivity for CDKL5 over CDKL2, low inhibition for CDKL3 and CDKL4 (IC50 = 2.1-2.7 ?M), and no inhibition for CDKL1. CAF 382 lacks GSK3β activity. It causes a significant reduction in pSer222 EB2 at 5 nM without a change in total EB2 levels in rat primary cortical neuron cultures. CAF 382 is an analog of SNS 032 (Cat. No. 4075).
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-164990 |
| Réf. fabricant | 30019005 |
| Nom chimique ou matériau | N-[5-[(5-Propan-2-yl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide trifluoroacetate |
| Quantité | 10 mg |
| Cible | CDKL5 |
| Formule moléculaire | C<sub>16</sub>H<sub>22</sub>N<sub>4</sub>O<sub>2</sub>S<sub>2</sub>.CF<sub>3</sub>CO<sub>2</sub>H |
| Pureté | 0.98 |
