SML4310
MS-275
≥98% (HPLC)
Synonym(s):
Entinostat, MS 27-275, SNDX 275, N-[[4-[[(2-Aminophenyl)amino]carbonyl]phenyl]methyl]-carbamic acid 3-pyridinylmethyl ester, (Pyridin-3-yl)methyl 4-(2-aminophenylcarbamoyl)benzylcarbamate
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About This Item
Empirical Formula (Hill Notation):
C21H20N4O3
CAS Number:
Molecular Weight:
376.41
UNSPSC Code:
12352200
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
General description
Orally available Class I HDAC inhibitor inducing histone hyperacetylation and gene reactivation, leading to anti-tumor, pro-apoptotic, and immunomodulatory outcomes.
MS-275 (Entinostat), a long-acting, orally bioavailable, cell-permeable, brain-region selective Class I HDACs (HDAC1 IC50 ~0.18-0.51 μM; HDAC3 IC50 ~0.74-1.7 μM) inhibitor 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.
MS-275 (Entinostat), a long-acting, orally bioavailable, cell-permeable, brain-region selective Class I HDACs (HDAC1 IC50 ~0.18-0.51 μM; HDAC3 IC50 ~0.74-1.7 μM) inhibitor 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.
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