Drug intelligence / Profile preview

MLS2438

Development stage
Preclinical
Lead developer
City of Hope
Modality
Small Molecules
01

Overview

MLS2438 is a novel 3′-substituted 7-bromoindirubin derivative that acts as a small-molecule inhibitor of STAT3 and AKT signaling pathways. It has been shown to directly inhibit the kinase activities of SRC and AKT both in vitro and in intact cancer cells. By suppressing these pathways, MLS2438 induces apoptosis in human melanoma cells and down-regulates anti-apoptotic proteins like Mcl-1 and pro-proliferative proteins like c-Myc. Preclinical studies in A2058 human melanoma xenograft mouse models demonstrated that MLS2438 suppresses tumor growth with low toxicity. It was developed through a collaboration between the City of Hope Cancer Center and the University of Athens.

Other names
3′-substituted 7-bromoindirubin derivative
02

Targets

GSK3 (Glycogen synthase kinase 3 beta)SFK (SRC family kinases)JAK (Janus kinase family)AKT (RAC-alpha serine/threonine-protein kinase)CDK (CDK family)

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