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About This Item
Empirical Formula (Hill Notation):
C21H20N4O3
CAS Number:
Molecular Weight:
376.41
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
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General description
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.
Application
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.
Biochem/physiol Actions
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.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Repr. 1A
Storage Class
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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