1354037-26-5

1354037-26-5 structure

Name: KH CB19
Chemical Name: (E)-ethyl 3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
CAS Number: 1354037-26-5
Molecular Formula: C₁₅H₁₃Cl₂N₃O₂
Molecular Weight: 338.18900
Catalog: Research Areas Cancer
Create Date: 2016-11-01 02:09:23
Modify Date: 2024-01-29 16:20:11
KH-CB19 is a potent and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).IC50 value: 20 nM (CLK1) [1]Target: CLK1/4 inhibitorin vitro: KH-CB19 showed potent inhibition of CLK1 with an IC50 of 20 nM, and for the pure isomer KH-CB19, almost 100-fold selectivity against the CLK3 isoform. Pretreatment of cells with KH-CB19 or TG003 led to a reduction of the TNF-α-induced increase in phosphorylation of all analyzed SR proteins compared with TNF-α-stimulated controls.Treatment of resting cells with 10 μM KH-CB19 significantly reduced the basal expression of flTF as well as asHTF [1].

Name	(E)-ethyl 3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
Synonyms	kh-cb19

Description	KH-CB19 is a potent and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).IC50 value: 20 nM (CLK1) [1]Target: CLK1/4 inhibitorin vitro: KH-CB19 showed potent inhibition of CLK1 with an IC50 of 20 nM, and for the pure isomer KH-CB19, almost 100-fold selectivity against the CLK3 isoform. Pretreatment of cells with KH-CB19 or TG003 led to a reduction of the TNF-α-induced increase in phosphorylation of all analyzed SR proteins compared with TNF-α-stimulated controls.Treatment of resting cells with 10 μM KH-CB19 significantly reduced the basal expression of flTF as well as asHTF [1].
Related Catalog	Research Areas >> Cancer
Target	CLK1:19.7 nM (IC50) CLK3:530 nM (IC50) DYRK1A:55.2 nM (IC50)
References	[1]. Fedorov O, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76. [2]. Grant SK, et al. Kinase inhibition that hinges on halogen bonds. Chem Biol. 2011 Jan 28;18(1):3-4.