Drug intelligence / Profile preview

KBH-A145

Development stage
Preclinical
Lead developer
Sungkyunkwan University
Modality
Small Molecules
Administration
Parenteral
01

Overview

KBH-A145 is a novel synthetic gamma-lactam-based hydroxamic acid derivative that acts as a histone deacetylase (HDAC) inhibitor. Developed by researchers at Sungkyunkwan University, the compound has demonstrated potent anticancer activity in preclinical models of breast and renal cancers. Mechanistically, KBH-A145 inhibits HDAC activity, particularly compromising the recruitment of HDAC1 to the p21 promoter, which leads to hyperacetylation of the promoter region and subsequent upregulation of the cyclin-dependent kinase inhibitor p21(WAF1/Cip1). This action induces G2/M phase cell cycle arrest and triggers apoptosis in sensitive cancer cell lines, such as MDA-MB-231 breast cancer cells, through the cleavage of poly(ADP-ribose) polymerase (PARP).

02

Targets

HDAC1 (Histone Deacetylase 1)

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