Drug intelligence / Profile preview

indirubin-3'-oxime-O-acetic acid

Development stage
Preclinical
Lead developer
Perha Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous, Topical, Oral
01

Overview

Indirubin-3'-oxime-O-acetic acid (I3MO) is a synthetic, water-soluble derivative of the natural alkaloid indirubin. It is characterized by the presence of a carboxymethyl group on the oxime moiety at the 3' position, which significantly improves its pharmacological profile compared to the parent indirubin. The compound acts as a potent, ATP-competitive inhibitor of several protein kinases, with high affinity for **glycogen synthase kinase-3 beta (GSK-3β)** and **cyclin-dependent kinases (CDKs)**, including CDK1 and CDK5. By inhibiting GSK-3β, it stabilizes β-catenin and activates Wnt signaling, a pathway crucial for stem cell maintenance and neuroprotection. Its inhibition of CDKs induces cell cycle arrest and apoptosis, positioning the compound as a research candidate for various cancers, including chronic myeloid leukemia. Due to its solubility and potency, it is widely utilized as a biochemical probe in the study of kinase-mediated signaling and cell cycle regulation.

Other names
2-({[(3E)-2'-oxo-1',2'-dihydro-3H-2,3'-biindol-3-ylidene]amino}oxy)acetic acid({[(3E)-2'-Oxo-2',7'-dihydro-2,3'-biindol-3(7H)-ylidene]amino}oxy)acetic acid
02

Targets

CDK2 (Cyclin-dependent kinase 2)CDK9 (Cyclin-dependent kinase 9)GSK3 (Glycogen synthase kinase 3 beta)JNK (Mitogen-activated protein kinase kinase kinase family)CDK1 (Cyclin-dependent kinase 1)CDK5 (Cyclin-dependent kinase 5)

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