bisthianostat

Bisthianostat is a novel, orally bioavailable small molecule that acts as a pan-inhibitor of human histone deacetylases (HDACs). It is based on a bisthiazole scaffold evolved from the thiazole–thiazoline cap group in the natural HDAC inhibitor largazole. Bisthianostat selectively binds to and inhibits HDACs, leading to increased acetylation of histone proteins. This results in chromatin remodeling, inhibition of tumor oncogene transcription, activation of tumor suppressor genes, cell cycle arrest, and apoptosis. Preclinical studies demonstrated antitumor activity in multiple myeloma models both as monotherapy and in combination with bortezomib. Early clinical trials indicate modest single-agent efficacy and good tolerability in patients with relapsed or refractory multiple myeloma[1][2][3][4][5][6].

Other names

bisthianostat