Drug intelligence / Profile preview

indirubin

Development stage
Unknown
Lead developer
Chang Gung Memorial Hospital
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Indirubin is a natural bisindole alkaloid derived from plants such as *Indigofera tinctoria* and *Isatis tinctoria*, and is the active component of traditional Chinese medicine formulas like Danggui Longhui Wan and Qing-Dai. It has been used clinically in Asia for the treatment of chronic myelogenous leukemia (CML) and other chronic diseases[1][4][7]. Indirubin exhibits anticancer, anti-inflammatory, and neuroprotective properties. Its primary mechanism of action involves potent ATP-competitive inhibition of cyclin-dependent kinases (CDKs) and glycogen synthase kinase-3 beta (GSK-3β), leading to cell cycle arrest at G2/M phase[4][5][6][8]. Indirubin also acts as a ligand for the aryl hydrocarbon receptor (AhR), modulating inflammation-associated signaling pathways including NF-kappaB, STAT3, TGF-beta, PI3K/AKT/mTOR, MAPK, JAK/STAT3[2][6][8]. Preclinical studies have demonstrated its efficacy against various cancers; clinical trials in China have shown activity against CML[5]. Poor water solubility limits its bioavailability; thus derivatives with improved pharmacological profiles are under investigation[8].

Other names
3,2'-bisindolebisindole alkaloid
02

Targets

Cyclin-dependent kinase 2–cyclin A or E complexGSK3 (Glycogen synthase kinase 3 beta)CDK4 (Cyclin-dependent kinase 4)CDK1 (Cyclin-dependent kinase 1)AHR (Aryl hydrocarbon receptor)

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