CLK1-IN-1

小分子

CLK1-输入-1

CLK1-IN-1

C656461-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM. In Vitro CLK1 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 Vivo APAP 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. IC50& Target:CLK1 2 nM (IC 50 )

CLK1-IN-1 是一种强效的 Cdc2 样激酶 1（CLK1）选择性抑制剂，其 IC 50 为 2 nM。

2123491-32-5(DMSO)

C24H16FN5O

409.42 g/mol

CC(C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6

包含CDK，MAPK，GSK3，CLK家族