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Compound 00229

Development stage: Preclinical
Lead developer: Tseng, T.
Modality: Small Molecules

Overview

Compound 00229 is a novel, hydrazide-based dual-target inhibitor that simultaneously targets tubulin and poly(ADP-ribose) glycohydrolase (PARG). Developed for the treatment of castration-resistant prostate cancer (CRPC), it exhibits potent antiproliferative activity, particularly in bone metastatic human mCRPC cell lines like PC-3, with an IC50 of 0.137 μM. The compound induces cell cycle arrest at the G2/M phase, associated with decreased cyclin D1 levels and altered cyclin A expression. Its mechanism of action involves inducing apoptosis through a combination of DNA damage (via PARG inhibition) and mitotic arrest (via tubulin inhibition). Preclinical data suggest its potential as a therapeutic candidate for advanced prostate cancer.

Targets

PARG (Poly(ADP-ribose) glycohydrolase)TUBB (Tubulin (alpha and beta subunits))

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