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CLK1-IN-3

Catalog No. T72039 CAS 2922550-28-3

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

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CLK1-IN-3, CAS 2922550-28-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 106.00
5 mg	In stock	$ 263.00
10 mg	In stock	$ 428.00
25 mg	In stock	$ 872.00
50 mg	In stock	$ 1,450.00
100 mg	In stock	$ 2,320.00

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Purity: 99.79%

Biological Description

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Description	Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).
Targets&IC50	CLK2:42 nM, CLK1:5 nM, DYRK1A:1521 nM, CLK4:108 nM
In vitro	CLK1-IN-3 (compound 10ad) demonstrates anti-tumor potential due to its dual inhibitory effects on Clk1 and Clk2[1]. CLK1-IN-3 (10 μM-1000 μM) effectively binds to the Clk1 protein and inhibits its degradation in a dose-dependent manner[1]. CLK1-IN-3 (0-10 μM, 24 h) induces autophagy in Hela, BNLCL.2, and HCT 116 cells[1]. CLK1-IN-3 stimulates the degradation of SQSTM1/p62 (autophagy marker)[1].
In vivo	CLK1-IN-3 (0-40 mg/kg, intraperitoneal injection, single dose) significantly inhibits acute liver injury induced by acetaminophen (APAP) in the ALI model, and there is no apparent hepatocyte death observed[1]. CLK1-IN-3 (10 mg/kg; intravenous injection, oral administration, intraperitoneal injection, single dose) exhibits acceptable pharmacokinetic characteristics, with a relatively long half-life (T1/2) of 5.29 hours and an oral bioavailability of 19.5%[1].

Molecular Weight	430.48
Formula	C24H23FN6O
CAS No.	2922550-28-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Yang T, et al. Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI). Eur J Med Chem. 2023 Mar 15;250:115168.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Autophagy Compound Library

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Keywords

CLK1-IN-3 2922550-28-3 Autophagy Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors DYRK CDK Benzamide,N[3(5fluoro3pyridinyl)1Hpyrrolo[2,3b]pyridin5yl]4(4methyl1piperazinyl) inhibitor inhibit

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