cdc-like

CLK-IN-T3 是 CLK1、CLK2 和 CLK3 的抑制剂，IC50 为 0.67、15 和 110 nM。 CLK-IN-T3 具有抗癌活性。

Cirtuvivint (SM08502) 是一种有效且具有口服活性的 CDC 样激酶 (CLK) 抑制剂，可用于研究关节炎。

MU1210 (compound 12f) 是一种针对CDC样激酶Clk1、Clk2和Clk4的抑制剂，其IC50分别为8、20和12 nM，对HIPK1和DYRK2的IC50分别为187和1309 nM。MU1210 还表现出良好的药代动力学特性（在小鼠中，10 mg kg，腹腔注射：Cmax=1.24 μM，T1 2=58分钟；未观察到急性毒性现象）。

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5 6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

CLK-IN-T3N 是 CLK-IN-T3 的阴性对照，是CLK 的探针。

SRI-29329 是一种有效的、特异性的 CDC 样激酶抑制剂，对 CLK1、CLK2 和 CLK4 的 IC50 分别为 78 nM、16 nM 和 86 nM。