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T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively.
T025 (0-1000 nM; 72 hours) significantly suppresses the growth of MDA-MB-468 cells in a dose-dependent manner. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation.
In Balb/c nude mice (7 to 8 week-old females), T025 (50 mg/kg; p.o.; 2, 4, 8 hours) suppress the CLK-dependent phosphorylation and induce skipping exon in various genes.
| Molecular Weight | 382.42 |
| Formula | C21H18N8 |
| CAS Number | 2407433-00-3 |
| Solubility (25°C) | DMSO 8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| ML 315
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. |
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