Drug intelligence / Profile preview

6-bromoindirubin-3'-oxime

Development stage
Preclinical
Modality
Small Molecules
01

Overview

6-bromoindirubin-3'-oxime is a hemi-synthetic derivative of indirubins found in edible mollusks and plants. It is a potent, selective, reversible, and ATP‐competitive small molecule inhibitor of glycogen synthase kinase‐3 beta (GSK‐3β) and also inhibits cyclin-dependent kinase complexes such as CDK1-cyclin B. The compound has demonstrated anti-tumor and anti-neurodegenerative activities in preclinical studies. Mechanistically, it reduces oxidative stress, activates cytoprotective cellular modules including antioxidant responses and proteostasis networks via Nrf2 activation, enhances autophagy through mTOR pathway inhibition, improves lipid metabolism in liver models of aging, suppresses cellular senescence-mediated biomolecular damage in human fibroblasts, and retards age-associated alterations[2][5]. Its pleiotropic effects are being explored for potential applications in cancer biology as well as neurodegeneration and metabolic diseases[5].

Other names
(2Z,3E)-6-Bromoindirubin-3'-oxime(2Z,3E)-6'-bromo-2,3'-biindole-2',3(1H,1'H)-dione 3-oximeBIOGSK 3B Inhibitor IXGSK3B Inhibitor IXGSK-3B Inhibitor IXCHEBI:86290
02

Targets

CDK1 (Cyclin-dependent kinase 1)GSK3 (Glycogen synthase kinase 3 beta)CDK5 (Cyclin-dependent kinase 5)

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