T025 |
Catalog No.GC65395 |
T025는 Cdc2와 유사한 키나아제 (CLKs)의 구체적인 억제제로, CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B 및 DYRK2에 대한 Kd 값이 각각 4.8 nM, 0.096 nM, 6.5 nM , 0.61 nM , 0.074 nM , 1.5n M 및32n M입니다.
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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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