CLK1-IN-1 (C09-1120-787)

CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM.In VitroCLK1 is the most potently inhibited kinase (IC 50 : 2 nM). In addition to CLK1, only two kinases have an IC 50 value less than 100 nM, namely CLK2 (IC 50 : 31 nM) and CLK4 (IC 50 : 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAPAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:CLK1 2 nM (IC 50 ). Specification: 0.99 Molecular Formula: C24H16FN5O Molecular Weight: 409.42 PubChem CID: 129318964 Isomeric SMILES: C[C@@H](C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6