Drug intelligence / Profile preview

T0070907

Development stage
Preclinical
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral
01

Overview

T0070907 is a **potent and selective small molecule antagonist of peroxisome proliferator-activated receptor gamma (PPARγ)**. It binds covalently to cysteine 313 in helix 3 of the PPARγ ligand binding domain, inhibiting its activity with high selectivity (demonstrating over 800-fold preference for PPARγ over PPARα and PPARδ)[4][5]. Mechanistically, T0070907 blocks recruitment of coactivators to PPARγ, promotes recruitment of corepressors (such as NCoR), and antagonizes agonist-induced PPARγ transcriptional activity[4]. It has demonstrated **anticancer effects**, including **cell cycle arrest (G2/M), inhibition of cell proliferation, and increased apoptosis**, primarily in cancer cell models such as breast, cervical, and colorectal cancers[1][2]. T0070907 also acts as a radiosensitizer in vitro, enhancing the effects of radiation therapy by inducing mitotic catastrophe in cancer cells[1]. Both PPARγ-dependent and -independent mechanisms have been reported for its antiproliferative action[1][2]. T0070907 is widely used as a chemical tool in preclinical research rather than as a therapeutic drug.

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)

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