CLK1-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CLK1-IN-3 (compound 10ad) 是一种有效的选择性 Clk1 抑制剂，其 IC50 为 5 nM，是 300 多倍 Dyrk1A 的选择性。CLK1-IN-3 对 Clk2 和 Clk4 也表现出相对有效的抑制作用，IC50 值分别为 42 和 108 nM。CLK1-IN-3 在体外有效诱导自噬 (autophagy)。CLK1-IN-3 可用于急性肝损伤 (ALI) 研究。

CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.

Western Blot AnalysisCell Line:Hela cells, BNLCL.2 and HCT 116 cells Concentration:0.2, 1, 5, and 10 μM Incubation Time:24 h Result:Elevated the expression level of LC3II protein (a marker of autophagosomes) as well as the ratio of LC3II to LC3I (a sensitive index of autophagy) in a dose-dependent and time-dependent manner.

Animal Model:Male C57BL/6 mice(8 weeks, injected acetaminophen (HY-66005) (500 mg/kg, ip))Dosage:10, 20, and 40 mg/kg Administration:IP, onceResult:Decreased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels significantly in dose-dependent.Animal Model:Male Balb/c mice (aged 8 weeks)Dosage:10 mg/kg Administration:IV, PO, IP, once (Pharmacokinetic Analysis) Result:Pharmacokinetic Parameters of CLK1-IN-3 in male Balb/C mice.

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Autophagy

Autophagy

Autophagy | DYRK | CDK

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2922550-28-3

430.48

C24H23FN6O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (232.30 mM; 超声助溶 )

O=C(NC=1C=NC=2NC=C(C=3C=NC=C(F)C3)C2C1)C4=CC=C(C=C4)N5CCN(C)CC5

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(-20℃)

With Ice Pack

≥ 2 years