Drug intelligence / Profile preview

KH-CB19

Development stage
Preclinical
Lead developer
ManRos Therapeutics
Modality
Small Molecules
01

Overview

KH-CB19 is a synthetic small molecule belonging to the indolecarboxylic acid derivatives class. It features a dichloro-substituted indole core with an (E)-2-amino-1-cyanoethenyl side chain and an ethyl carboxylate ester. The compound acts as a potent inhibitor of CDC-like kinases (CLKs), particularly dual specificity protein kinase CLK1. By inhibiting CLK family kinases involved in alternative pre-mRNA splicing regulation, KH-CB19 modulates splicing events implicated in cancer and neurodegenerative diseases. Structural studies have shown its binding to the kinase domain of human CLK1 and CLK3[4][6][7]. Preclinical research suggests anticancer activity through inhibition of cell proliferation and induction of apoptosis in cancer cell lines[4].

Other names
ethyl 3-[(E)-2-amino-1-cyanoethenyl]-6,7-dichloro-1-methylindole-2-carboxylateethyl 3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
02

Targets

CLK4CLK3 (CDC-like kinase 3)CLK1 (CDC-like kinase 1)

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