Givinostat CAS# 497833-27-9 [4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯

Givinostat (ITF-2357) is a hydroxamic acid-based histone deacetylase (HDAC) inhibitor with potent anti-inflammatory and antineoplastic activity. It selectively inhibits class I and II HDACs, leading to accumulation of acetylated histones, modulation of gene expression, and apoptosis in malignant cells. In vitro, Givinostat has demonstrated IC₅₀ values in the low nanomolar range for HDAC1 (10 nM) and HDAC2 (7.5 nM), with minimal activity against class III HDACs. It effectively suppresses pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in monocytes and macrophages. Clinically, it has shown efficacy in hematological malignancies, particularly polycythemia vera, where it reduces JAK2^V617F allele burden and improves hematologic parameters.