Drug intelligence / Profile preview

GW8510

Development stage
Unknown
Modality
Small Molecules
Administration
Intraperitoneal, Intramuscular
01

Overview

GW8510 is a cyclin-dependent kinase 2 (CDK2) inhibitor that has been investigated for multiple therapeutic applications. Originally developed as a CDK2 inhibitor, subsequent research has shown it to be non-selective. The compound works through multiple mechanisms including promoting proteasomal degradation of ribonucleotide reductase M2 (RRM2), activating p53 transcriptional activity, and inducing autophagic cell death. GW8510 has demonstrated potential therapeutic effects in **muscle atrophy** by activating the AMPK/PGC1α pathway, improving muscle function, and reducing oxidative stress. In **colorectal cancer**, it exhibits anti-cancer effects through RRM2 inhibition and autophagy induction, working independently of p53 status. The compound also increases insulin expression in pancreatic alpha cells through p53-dependent mechanisms involving JNK and p38 pathways. Additionally, GW8510 has shown neuroprotective effects by suppressing neuronal apoptosis. The compound induces G2/M cell cycle arrest and has been explored for potential repositioning in various disease contexts including pancreatic cancer, breast cancer, and Parkinson's disease.

02

Targets

RRM2CDK2 (Cyclin-dependent kinase 2)

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