KH CB19

Modify Date: 2024-01-29 16:20:11

KH CB19 Structure
KH CB19 structure
Common Name KH CB19
CAS Number 1354037-26-5 Molecular Weight 338.18900
Density N/A Boiling Point N/A
Molecular Formula C15H13Cl2N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of KH CB19


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].

 Names

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

 KH CB19 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C15H13Cl2N3O2
Molecular Weight 338.18900
Exact Mass 337.03800
PSA 81.04000
LogP 4.18528
Storage condition 2-8℃

 Synonyms

kh-cb19
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