MS-275

MS-275 belongs to the class of 2-aminophenyl benzamides. It is a long-acting, orally bioavailable, cell-permeable, brain-region selective Class I Histone Deacetylases (HDACs) inhibitor.

MS-275 is suitable for use in nano-formulation and encapsulation to study its anticancer activity.It may be used to study its therapeutic effect and regulatory mechanism in angiotensin (Ang) II-induced hypertensive mice.

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.