Nutrabiotech Entinostat MS-275 1.2G Powder, 98% high purity Entinostat MS-275 powder, selective Class I HDAC1/2/3 inhibitor, epigenetic regulator, tumor cell apoptosis research raw material

CAS 209783-80-2 MS-275 Entinostat Powder Oral HDAC Inhibitor for Epigenetic Cancer Pharmacology Research

High-purity MS-275 (Entinostat) powder CAS 209783-80-2 is a potent, orally bioavailable benzamide-based selective class I HDAC inhibitor. It exhibits high selectivity for HDAC1 and HDAC3 with nanomolar IC50 values, effectively promoting histone hyperacetylation, relaxing chromatin structure and reactivating silenced tumor suppressor genes. This epigenetic regulator induces cancer cell cycle arrest, cell differentiation and apoptosis, inhibits tumor proliferation and reprograms cellular metabolism to suppress tumor growth. Widely applied in laboratory research of breast cancer, liver cancer, leukemia, ovarian carcinoma, epigenetic mechanism exploration, immunotherapy combination study and targeted anti-tumor drug screening. All batches pass strict HPLC purity testing, with customized packaging and global bulk supply available for oncology and epigenetic pharmacology laboratories. For scientific research use only.
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Entinostat (CAS 209783-80-2) Class I HDAC Inhibitor | SNDX-275 / MS-275, HDAC1/HDAC3 Epigenetic Anti-Cancer Compound

Entinostat CAS 209783-80-2
Class I HDAC Inhibitor (SNDX-275, MS-275)

Entinostat (CAS 209783-80-2), also SNDX-275 / MS-275, is an orally bioavailable benzamide inhibitor of class I histone deacetylases HDAC1 and HDAC3 (IC50 ~0.18-0.51 and ~0.74-1.7 uM respectively), with selectivity over HDAC8. By restoring histone acetylation it reactivates silenced tumor-suppressor genes and modulates the immune microenvironment. Molecular formula C21H20N4O3, MW 376.41. Research-grade with COA.

HDAC Inhibitor Class I HDAC HDAC1/HDAC3 Epigenetics SNDX-275 MS-275 Anti-Cancer Breast Cancer
Request a Quote Technical Specs
376.41
MW (C21H20N4O3)
≥98%
Purity (HPLC)
HDAC1/3
Class I selective

Molecular Information

Name: Entinostat
CAS: 209783-80-2
Formula: C21H20N4O3
MW: 376.41 g/mol
Class: Benzamide HDAC inhibitor
Core: (2-aminophenyl)benzamide carbamate
Target: Class I HDAC (HDAC1/HDAC3)
IC50: HDAC1 0.18-0.51 uM
MP: 159-160 C
Appearance: White to beige powder
Synonyms: SNDX-275 / MS-275
Storage: -20 C
🧪
CAS Number
209783-80-2
⚖️
Molecular Weight
376.41
🎯
Primary Activity
Class I HDAC Inhibitor
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Entinostat (CAS 209783-80-2)

📋 Physicochemical Properties

  • Product NameEntinostat (SNDX-275 / MS-275)
  • IUPAC Corepyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
  • CAS Number209783-80-2
  • SynonymsSNDX-275; MS-275; MS 27-275; NSC-706995
  • Molecular FormulaC21H20N4O3
  • Molecular Weight376.41 g/mol
  • SourceSynthetic small molecule (Syndax)
  • AppearanceWhite to beige powder
  • Melting Point159-160 C
  • Water SolubilityVery low
  • Organic SolubilityDMSO ~38 mg/mL; ethanol ~2 mg/mL
  • Compound Class2-aminophenyl benzamide / class I HDAC inhibitor
  • HS Code2933.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormCrystalline powder
  • Primary TargetClass I HDAC (HDAC1, HDAC3)
  • Pathway ReadoutHistone H3/H4 acetylation; re-activated transcription
  • SelectivityHDAC1/HDAC3 >> HDAC8 (IC50 >100 uM)
  • Storage Condition-20 C, sealed, protect from light
  • Solution StabilityDMSO stock stable ~1 week at -20 C
  • ShippingBlue ice / cold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Nodes

Entinostat's reach is the epigenetic machinery and the transcriptional programs — plus the immune microenvironment — that HDAC1/HDAC3 tone controls.

🧬 HDAC1 (class I) 🧬 HDAC3 (class I) 🧾 Histone H3 / H4 Acetylation 🧬 HDAC8 (not inhibited) ⚙️ Chromatin Remodeling 🧱 Transcription Factors (access) 🛡️ Tumor Microenvironment 🔥 Treg / Immune Modulation 🧬 ER / Hormone Signaling 🧫 Apoptosis & Differentiation 🧬 Epigenetic Silencing 🔬 p21 / p27 Induction

How Entinostat Works: Reopening Silent Chromatin

Entinostat blocks class I HDACs, letting histones stay acetylated so repressed genes can be read

1

HDAC1/HDAC3 Catalytic Blockade

Entinostat binds the catalytic zinc pocket of class I HDACs, preferentially inhibiting HDAC1 (IC50 ~0.18-0.51 uM) and HDAC3 (~0.74-1.7 uM), while sparing HDAC8 (IC50 >100 uM). This stops removal of acetyl groups from lysine residues on histone tails.

2

Histone Hyperacetylation & Open Chromatin

With deacetylation blocked, histones H3 and H4 accumulate acetyl marks, weakening histone-DNA interaction and converting compact heterochromatin toward transcriptionally permissive euchromatin. Promoters previously locked by HDAC-driven silencing become accessible to the transcription machinery.

3

Reactivation, Cell-Cycle Arrest & Immune Modulation

Re-expressed tumor-suppressor and differentiation genes drive G1 arrest, apoptosis and differentiation. Clinically, entinostat also remodels the tumor microenvironment — reducing regulatory T cells and enhancing anti-tumor immunity — which underlies its synergy with endocrine therapy and immune approaches.

⚖️ Entinostat vs Vorinostat vs Romidepsin

  • Entinostat (this product)Class I (HDAC1/3) benzamide; oral; long half-life
  • Vorinostat (SAHA)Pan-HDAC (class I + II) hydroxamate
  • RomidepsinClass I (HDAC1/2) natural depsipeptide
  • HDAC8Entinostat sparing; others vary
  • Selectivity EdgeClass I focus reduces some pan-HDAC toxicities
  • Combination NicheEndocrine & immune combination partner

♻️ Downstream Biological Consequences

  • ChromatinHistone H3/H4 hyperacetylation
  • TranscriptionReactivation of silenced suppressor genes
  • Cell CycleG1 arrest; p21/p27 induction
  • SurvivalApoptosis & differentiation in tumor cells
  • ImmuneTreg reduction; enhanced anti-tumor response
  • Hormone AxisSensitization to endocrine therapy

Research Applications & Models

Entinostat is a founder of epigenetic combination therapy — from breast cancer to NSCLC and the emerging immuno-epigenetics field.

🎀

Breast Cancer & Endocrine Therapy

Studied with aromatase inhibitors and fulvestrant in hormone-receptor-positive metastatic breast cancer, where HDAC inhibition re-sensitizes resistant clones (e.g., the ENCORE 301 paradigm). A flagship epigenetic-combination model.

HR+ BC
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Non-Small-Cell Lung Cancer

Investigated with EGFR and chemotherapy backbones and, increasingly, with immunotherapy, to overcome epigenetic silencing of immune and tumor-suppressor programs in NSCLC.

NSCLC
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Epigenetic Reactivation Studies

A reference class I HDAC inhibitor for chromatin immunoprecipitation, histone-acetylation Western panels and reporter assays probing silenced-gene re-expression.

Chromatin
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Immuno-Oncology & Treg Modulation

Explored for reducing regulatory T-cell suppressive activity and improving checkpoint-inhibitor responses — the growing field of epigenetic priming of immunity.

Treg / IO
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Differentiation & Apoptosis Models

Used to induce myeloid differentiation and apoptosis in leukemic and solid-tumor lines, leveraging HDAC1/HDAC3 control of differentiation programs.

Differentiation
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HDAC Selectivity Profiling

Benchmarked against pan-HDAC and class-I/II agents to map which HDAC isoforms drive specific phenotypes — important for isoform-selective drug discovery.

HDAC Isoforms
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Combination Screening

Deployed with hormonal, cytotoxic and immune agents to find synergy and overcome acquired resistance via chromatin remodeling.

Combo Matrix
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Aging & Senescence Research

HDAC inhibition modulates cellular senescence and stress responses; entinostat is used in models of senescence-associated secretory phenotype and age-related epigenetic drift.

Senescence

Key Literature & Landmark Publications

Landmark papers on HDAC inhibition and entinostat clinical translation.

Marks PA, Richon VM, Rifkind RA. Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells. J Cell Biochem. 2000;76(2):190-9. (HDACi biology).
Landmark reference
Yardley DA, et al. Randomized phase II, double-blind, placebo-controlled study of exemestane with or without entinostat in postmenopausal women with hormone receptor-positive metastatic breast cancer. J Clin Oncol. 2013;31(17):2128-35. (ENCORE 301).
doi: 10.1200/JCO.2012.46.1309
Rosato RR, Grant S. Histone deacetylase inhibitors in cancer therapy. (review of entinostat-class agents).
Landmark reference
SNDX-275 / MS-275 investigator reports. Entinostat in NSCLC and combination studies. (clinical program).
Landmark reference
Dokmanovic M, et al. Histone deacetylase inhibitors: overview and perspectives. (HDAC isoform selectivity).
Landmark reference

Available Sizes & Ordering

Research-grade Entinostat (CAS 209783-80-2) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard1gIn StockHDAC / epigenetic cell assaysSame/next-day ship
Medium5gIn StockIn vivo tumor & combination modelsSame/next-day ship
Large10gIn StockChromatin & immuno-oncology studiesSame/next-day ship
Bulk100gIn StockFormulation & process developmentQuote to confirm
Industrial1KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is entinostat and what does it inhibit?
Entinostat (CAS 209783-80-2), also SNDX-275 / MS-275, is a benzamide inhibitor of class I histone deacetylases, preferentially HDAC1 (IC50 ~0.18-0.51 uM) and HDAC3 (~0.74-1.7 uM), with little activity against HDAC8 (IC50 >100 uM). It is an orally bioavailable epigenetic anti-cancer agent. Formula C21H20N4O3, MW 376.41.
How does an HDAC inhibitor work as an anti-cancer agent?
HDACs remove acetyl groups from histones, compacting chromatin and silencing genes — including tumor suppressors. Entinostat blocks HDAC1/HDAC3, so histones H3/H4 become hyperacetylated, chromatin opens, and silenced genes (suppressors, differentiation factors) are re-expressed. The downstream effect is G1 arrest, apoptosis and differentiation, plus remodeling of the immune microenvironment.
Why is entinostat studied with endocrine therapy?
In hormone-receptor-positive breast cancer, epigenetic silencing can drive resistance to aromatase inhibitors and fulvestrant. Entinostat reverses aspects of that silencing and, in the ENCORE 301 paradigm, improved outcomes when added to exemestane — making it a founder of epigenetic combination therapy.
What distinguishes entinostat from vorinostat or romidepsin?
Vorinostat (SAHA) is a pan-HDAC (class I + II) hydroxamate; romidepsin is a class I (HDAC1/2) depsipeptide; entinostat is a class I (HDAC1/HDAC3) benzamide with oral bioavailability and a long half-life, and it spares HDAC8. This narrower isoform focus is thought to shape its efficacy and tolerability profile and its combination behavior.
What readouts confirm HDAC inhibition?
The canonical readout is histone H3 and H4 acetylation by Western blot or flow cytometry, plus re-expression of silenced reporters/genes and induction of cell-cycle inhibitors p21/p27. Acetyl-tubulin can also rise (class IIb HDAC6 cross-talk depending on concentration).
How soluble is entinostat and how should it be prepared?
Entinostat is soluble in DMSO (~38 mg/mL) and ethanol (~2 mg/mL), poorly in water. For cell assays dilute the DMSO stock into medium (final DMSO ≤0.1% v/v); active concentrations are typically sub-micromolar to low micromolar. Store solid at -20 C; DMSO stock is stable about a week at -20 C. Aliquot to avoid freeze-thaw.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, NMR structural confirmation and MS data. MSDS/SDS, residual-solvent data and Certificates of Origin are available on request. Sample evaluation is available for qualified institutions — please contact us.

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Research-grade Entinostat (CAS 209783-80-2) — purity ≥98% HPLC, COA included
SNDX-275 / MS-275 — the HDAC1/HDAC3 epigenetic agent that reopens silenced chromatin — request a quote today

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Weight 1 g

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