CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
体外研究
CLK-IN-T3 inhibits DYRK1A (IC50=260 nM) and DYRK1B (IC50=230 nM).
CLK-IN-T3 (0.1-10.0 µM; 24 hours) results in mild cell cycle arrest at the G2/M boundary with long-duration (24 h).
CLK-IN-T3 (0.5-1.0 µM; 6 hours) decreases phosphorylation of CLK-targeted SR proteins and CLK proteins increase slightly.
Cell Cycle Analysis
Cell Line:
HCT-116 cells
Concentration:
0.1, 0.5, 1.0, 5.0, 10.0 µM
Incubation Time:
24 hours
Result:
Resulted in mild cell cycle arrest at the G2/M boundary with long-duration (24 h).
Western Blot Analysis
Cell Line:
HCT-116 cells
Concentration:
0.5, 1.0 μM
Incubation Time:
6 hours
Result:
Decreased phosphorylation of CLK-targeted SR proteins and CLK proteins increased slightly.
分子式
C28H30N6O2
分子量
482.58
CAS号
2109805-56-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 4.83 mg/mL (10.01 mM; Need ultrasonic and warming)