Drug intelligence / Profile preview

kenpaullone

Development stage
Preclinical
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
Administration
Intraperitoneal, Intrathecal, Intracochlear
01

Overview

**Kenpaullone** is a small molecule kinase inhibitor primarily targeting **glycogen synthase kinase 3 beta (GSK-3β)** with an IC50 of 0.23 μM, alongside inhibition of cyclin-dependent kinases (CDKs) such as CDK1 (IC50 0.4 μM), CDK2 (IC50 0.68-7 μM), and CDK5 (IC50 0.85 μM), as well as HGK and Lck. It exhibits anti-inflammatory, immunomodulatory, and neuroprotective effects, and has been investigated in preclinical models for enhancing temozolomide efficacy in glioblastoma by targeting glioma stem cells, ameliorating neuropathic pain via upregulation of KCC2 expression, attenuating amyloid-beta deposition in Alzheimer's disease, promoting motor neuron survival in ALS models, and protecting against cisplatin-induced hearing loss. Kenpaullone also supports induced pluripotent stem cell generation by replacing Klf4 in reprogramming cocktails. Its chemical formula is C16H11BrN2O (MW 327.18, CAS 142273-20-9), and it is available as a research tool from suppliers like LKT Labs, R&D Systems, Sigma-Aldrich, and TCI.[1][2][4][7][10][12][13][17]

Other names
9-Bromopaullone9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one
02

Targets

CDK2 (Cyclin-dependent kinase 2)GSK3 (Glycogen synthase kinase 3 beta)CDK1 (Cyclin-dependent kinase 1)CDK5 (Cyclin-dependent kinase 5)

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