Sigma-Aldrich MS-275，≥98%（HPLC），粉末，HDAC抑制剂

产品概述

MS-275属于2-氨基苯基苯甲酰胺类药物，是一种长效、口服生物利用度高、细胞渗透性强、脑区选择性的I类组蛋白去乙酰化酶（HDACs）抑制剂。

应用领域

MS-275适合于纳米制剂和微囊化研究其抗肿瘤活性，可用于研究其对血管紧张素II（Ang II）诱导的高血压小鼠的治疗作用及其调节机制。

生化/生理作用

MS-275 (Entinostat), a Class I Histone Deacetylases HDACs (HDAC1 IC50 ~0.18-0.51 μM; HDAC3 IC50 ~0.74-1.7 μM) inhibitor, acts via reversible active site zinc binding. This inhibition induces histone hyperacetylation, promoting euchromatin formation and DNA accessibility to transcription factors, which reactivates silenced tumor suppressor and cancer-associated genes, mediating anti-proliferative, pro-apoptotic, and differentiation-inducing effects, ultimately inhibiting cancer cell growth and survival (IC50 ~0.0415-1.92 μM in human tumor cell lines). Furthermore, MS-275 demonstrates significant in vivo antitumor activity (e.g., 5 mg/kg), exhibits immunomodulation including Treg suppression, sensitizes cancer cells to other therapies, and modulates the tumor microenvironment.

技术规格