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SB415286

Development stage: Preclinical
Lead developer: GSK
Modality: Small Molecules
Administration: Intraperitoneal

Overview

SB415286 is a potent and selective small molecule inhibitor of glycogen synthase kinase-3 (GSK3), targeting both the alpha (GSK3α) and beta (GSK3β) isoforms. Developed by GSK, it functions as an ATP-competitive inhibitor. Research, such as that presented at AACR 2013, indicates that SB415286 can sensitize acute myeloid leukemia (AML) cells to Vitamin D-mediated differentiation by modulating the Vitamin D receptor (VDR) and its interactions with co-regulators like NcoR and SRC-3. Beyond oncology, SB415286 has been utilized as a pharmacological tool to study GSK3's role in neuroprotection, glucose metabolism, and various signaling pathways including Wnt/β-catenin.

Other names: 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione

Targets

GSK3 (Glycogen synthase kinase 3 beta)

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