Drug intelligence / Profile preview

CPTH6

Development stage
Preclinical
Modality
Small Molecules
Administration
In Vitro, In Vivo
01

Overview

CPTH6 is a thiazole derivative small molecule that acts as a specific inhibitor of lysine acetyltransferase activity, targeting the histone acetyltransferases Gcn5 and pCAF, but not p300 or CBP. It induces histone H3 and H4 hypoacetylation and reduces α-tubulin acetylation in multiple cancer cell types. CPTH6 promotes cell cycle arrest, apoptosis through mitochondrial pathways, and impairs autophagy via effects on ATG7-dependent autophagosomal membrane formation. It preferentially targets cancer stem-like cells, particularly lung cancer stem-like cells (LCSCs), inhibiting in vitro and in vivo tumor growth and reducing self-renewal and stemness markers. CPTH6 also inhibits angiogenesis, affecting vascular network formation and VEGF/VEGFR2 pathways. Its activity has been demonstrated in acute myeloid leukemia, lung cancer, and other solid tumors[1][2][5][6][7][8].

Other names
3-methylcyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl]hydrazone
02

Targets

KAT2A (Lysine acetyltransferase 2A)KAT2B

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