T025 |
Catalog No.GC65395 |
T025 est un inhibiteur par voie orale et hautement puissant de la kinase de type Cdc2 (CLK), avec des valeurs Kd de 4,8, 0,096, 6,5, 0,61, 0.074, 1.5 et 32 nM pour CLK1 , CLK2 , CLK3 , CLK4 , DYRK1A , DYRK1B et DYRK2 respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2407433-00-3
Sample solution is provided at 25 µL, 10mM.
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 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research[1].
T025 (0-1000 nM; 72 hours) significantly suppresses the growth of MDA-MB-468 cells in a dose-dependent manner[1].T025 (0-1000 nM; 6 hours) reduces phosphorylation levels in MDA-MB-468 cells[1].
T025 (50 mg/kg; p.o.; 2, 4, 8 hours, Balb/c nude mice (7 to 8 week-old females).) suppress the CLK-dependent phosphorylation and induce skipping exon in various genes[1]. T025 (50 mg/kg; p.o.; twice daily on 2 days per week, for 3 weeks, Balb/c nude mice (7 to 8 week-old females).) inhibits MDA-MB-468 xenograft mice tumor growth and without affect body weight [1].
[1]. Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6):e8289.
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