Drug intelligence / Profile preview

6-bromoindirubin-3'-acetoxime

Development stage
Preclinical
Lead developer
Phosphorex
Modality
Small Molecules
Administration
Intravenous, Subcutaneous, Oral, Intraperitoneal
01

Overview

6-Bromoindirubin-3'-acetoxime (BiA) is a synthetic small molecule derivative of indirubin, a natural compound found in indigo plants and the Mediterranean mollusk *Hexaplex trunculus*. It acts as a potent, ATP-competitive protein kinase inhibitor with a broad selectivity profile, primarily targeting glycogen synthase kinase-3 (GSK-3), Src-family kinases, and JAK2. BiA has been investigated for its therapeutic potential in oncology, particularly for glioblastoma (GBM) and pediatric diffuse midline glioma (DMG), where it has shown the ability to modulate the blood-brain barrier, inhibit tumor cell migration, and exert anti-angiogenic effects. Additionally, the compound has demonstrated antiviral activity against herpes simplex virus-1 (HSV-1) and varicella zoster virus. To address its poor solubility and bioavailability, a nanoparticle formulation known as PPRX-1701 was developed by Phosphorex, which has shown preclinical efficacy in brain tumor models by downregulating immunosuppressive pathways such as IDO1.

Other names
6-bromoindirubin-3'-acetoxime
02

Targets

CDK (CDK family)JAK2 (Janus kinase 2)GSK3 (Glycogen synthase kinase 3 beta)SFK (SRC family kinases)

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