CLK1-IN-1

Name: CLK1-IN-1
Brand: TargetMol
SKU: T10836
Price: 138 USD
Availability: InStock
Rating: 4.5 (1 reviews)

产品编号 T10836Cas号 2123491-32-5

CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).

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产品编号 T10836Cas号 2123491-32-5

CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).

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产品介绍

生物活性

产品描述	CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).
靶点活性	CLK1:2 nM
体外活性	In addition to CLK1, only two kinases have an IC50 value less than 100 nM, namely CLK2 (IC50: 31 nM) and CLK4 (IC50: 8 nM), DYRK1A is the strongest off-target. 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 stimulates the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate induction of autophagic flux by CLK1-IN-1.
体内活性	APAP exposure results in severe liver injury and treatment with CLK1-IN-1 (i.p., 30 mg/kg) imparts a significant hepatoprotective effect. Treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels.

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 25 mg/mL (61.06 mM), Sonication is recommended.

溶液配制表

DMSO