Drug intelligence / Profile preview

JKA97

Development stage
Preclinical
Lead developer
University of Tennessee
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

JKA97 is a novel synthetic benzylidene analog of harmine (a beta-carboline alkaloid) that exhibits potent anti-cancer activity. It has been shown to inhibit the growth and proliferation of various cancer cell lines, including breast, colon, and liver cancers, both in vitro and in vivo. Mechanistically, JKA97 induces G1 cell cycle arrest and apoptosis. It up-regulates the cyclin-dependent kinase inhibitor p21 (WAF1/CIP1) and p27 at the transcriptional level in a p53-independent manner, while down-regulating cyclin D1 and cyclin E. Additionally, JKA97-induced apoptosis is associated with Bax translocation and activation of the mitochondrial apoptotic pathway.

Other names
1-styryl-9H-pyrido(3,4-b)indolebenzylidene harminemethoxy-1-styryl-9H-pyrido-[3,4-b]-indolemethoxy-1-styryl-9H-pyrido[3,4-b]indole
02

Targets

BAX (Apoptosis regulator BAX)CCND1 (Cyclin D1)CCNE1 (Cyclin E1)CDKN1B (Transmembrane emp24 domain-containing protein 7)

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