CLK-IN-T3是一种高效，选择性和稳定的CDC样激酶(CLK)抑制剂，对CLK1，CLK2和CLK3蛋白激酶的IC50分别为0.67nM，15nM和110nM。CLK-IN-T3具有抗癌活性。
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[1].
CLK-IN-T3 inhibits DYRK1A (IC50=260 nM) and DYRK1B (IC50=230 nM)[1]. 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)[1]. CLK-IN-T3 (0.5-1.0 µM; 6 hours) decreases phosphorylation of CLK-targeted SR proteins and CLK proteins increase slightly[1]. Cell Cycle Analysis[1] Cell Line: HCT-116 cells
[1]. Funnell T, et al. CLK-dependent exon recognition and conjoined gene formation revealed with a novel smallmolecule inhibitor. Nat Commun. 2017 Feb 23;8(1):7.
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