Entinostat (MS-275)

Catalog No.S1053

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Phase 3.

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Entinostat (MS-275) Chemical Structure

Entinostat (MS-275) Chemical Structure
Molecular Weight: 376.41

Validation & Quality Control

Cited by 57 publications:

14 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Entinostat (MS-275) is available in the following compound libraries:

HDAC Inhibitors with Unique Features

Product Information

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Product Description

Biological Activity

Description Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Phase 3.
Targets HDAC1 [2]
(Cell-free assay)
HDAC3 [2]
(Cell-free assay)
IC50 0.51 μM 1.7 μM
In vitro MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. [1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. [2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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... Click to View More Cell Line Experimental Data

In vivo MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. [4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. [5]
Features

Protocol(Only for Reference)

Kinase Assay:

[6]

Standard HDAC Assays Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.

Cell Assay:

[2]

Cell lines A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells
Concentrations ~ 10 μM
Incubation Time 3 days
Method

Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.

Animal Study:

[1]

Animal Models A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.
Formulation Dissolved with 0.05 N HCl, 0.1% Tween 80
Dosages 12.3, 24.5 and 49 mg/kg
Administration Administered orally once daily 5 days per week for 4 weeks

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Saito A, et al. Proc Natl Acad Sci U S A, 1999, 96(8), 4592-4597.

[2] Sugawara T, et al. 95th AACR, Orlando, 2004, Abst#2451

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02780804 Not yet recruiting Childhood Brain Stem Neoplasm|Childhood Lymphoma|Childhood Solid Neoplasm|Pineal Region Neoplasm|Recurrent Childhood Central Nervous System Neoplas  ...more Childhood Brain Stem Neoplasm|Childhood Lymphoma|Childhood Solid Neoplasm|Pineal Region Neoplasm|Recurrent Childhood Central Nervous System Neoplasm|Recurrent Childhood Visual Pathway Glioma|Refractory Central Nervous System Neoplasm National Cancer Institute (NCI) March 2017 Phase 1
NCT02697630 Not yet recruiting Metastatic Uveal Melanoma Vastra Gotaland Region|Merck Sharp & Dohme Corp.|Syndax P  ...more Vastra Gotaland Region|Merck Sharp & Dohme Corp.|Syndax Pharmaceuticals June 2016 Phase 2
NCT02708680 Not yet recruiting Breast Cancer Syndax Pharmaceuticals|Roche Pharma AG April 2016 Phase 1|Phase 2
NCT02453620 Recruiting Breast Adenocarcinoma|HER2/Neu Negative|Invasive Breast Carcinoma|Recurrent Breast Carcinoma|Solid Neoplasm|Stage IIIA Breast Cancer|Stage IIIB Bre  ...more Breast Adenocarcinoma|HER2/Neu Negative|Invasive Breast Carcinoma|Recurrent Breast Carcinoma|Solid Neoplasm|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer National Cancer Institute (NCI) November 2015 Phase 1
NCT02437136 Recruiting Non-Small Cell Lung Cancer|Melanoma Syndax Pharmaceuticals|Merck Sharp & Dohme Corp. July 2015 Phase 1|Phase 2

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Chemical Information

Download Entinostat (MS-275) SDF
Molecular Weight (MW) 376.41
Formula

C21H20N4O3

CAS No. 209783-80-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms SNDX-275
Solubility (25°C) * In vitro DMSO 75 mg/mL (199.25 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate

Customer Product Validation(14)


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Source PLoS Biol 2014 12, e1001758. Entinostat (MS-275) purchased from Selleck
Method WST-1 assay, Propidium iodide staining
Cell Lines U87 cells
Concentrations 1 uM
Incubation Time 4 days
Results IFNLR1 up-regulation by HDAC inhibitors renders cancer cells sensitive to the antitumor properties of IFN-λ. In accordance with hypothesis, combined treatment of U87 glioblastoma cells with MS-275 and IFN-λ inhibited growth in culture over a 4-d time course, while IFN-λ alone had minimal effects on proliferation (A, B). It employed a three-dimensional spheroid culture system to mimic physiological conditions of tumor growth. Consistently, the combined treatment reduced both the size and number of U87 spheroid formation (C–E). WST-1 assay in the 3D culture also revealed reduced glioblastoma proliferation following the combination treatment (F).

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Source J Neurosci 2011 31, 3990-9. Entinostat (MS-275) purchased from Selleck
Method Glutamate assay
Cell Lines HDACs
Concentrations 1 uM
Incubation Time 30 min
Results Exposing MONs to OGD resulted in a loss of adenomatus polyposis coli (APC (+)) oligodendrocytes and a gain in the appearance of pyknotic nuclei with brighter Sytox fluorescence in MONs imaged 5 h after 60 min of OGD (white arrows). Treatment of MONs with SAHA (1 uM) or MS-275 (1 uM) preserved oligodendrocyte numbers (64.6 ?2.1% and 63.5 ?1.9%, n=6, p<0.001, one-way ANOVA), ameliorated axonal neurofilament loss, and reversed APC (+) cell loss and kept pyknotic nuclei counts to the level observed under control conditions.

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Source Sci Signal 2010 3, ra80. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines HAUSP WT cells, HAUSP KO cells, HEK 293 cells, RKO cells
Concentrations 5 μM
Incubation Time 24/48/72 h
Results The HDAC inhibitor MS-275 directly destabilizes DNMT1 by enhancing its ubiquitination (Fig. A and B).We then showed that acetylation of DNMT1 plays a direct role in this process. HDAC Inhibitor MS-275 increased DNMT1 acetylation (Fig.C). The functional importance of DNMT1 acetylation was then demonstrated by showing that inhibition of HDAC activity failed to induce degradation of a DNMT1 mutant in which the four previously identified acetylated lysines were altered to arginines (Fig. D). inducible knockdown of HDAC1 in RKO colorectal cancer cells led to reduced DNMT1 abundance, consistent with a similar observation made in a breast cancer cell line (Fig. E). Knockdown of HDAC1 led to increased DNMT1 acetylation (Fig. 2F). These data suggest that HDAC1 deacetylates DNMT1, thus protecting it from proteasomal degradation.

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Source Sci Signal 2010 3, ra80. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines HEK 293 cells
Concentrations 5 μM
Incubation Time 24 h
Results HDAC inhibitor MS-275 increased the interaction between endogenous and transfected DNMT1 and UHRF1 (Fig. A to C). Furthermore, overexpression of UHRF1 led to increased ubiquitination of DNMT1 (Fig. D). UHRF1-mediated ubiquitination was required for HDAC inhibitor(MS-275)-induced degradation of DNMT1. In addition, knockdown of UHRF1 by three different siRNAs blocked HDAC inhibitor-induced degradation of DNMT1 (Fig. E). Conversely, overexpression of UHRF1 reduced the abundance of a DNMT1 mutant lacking the HAUSP interaction domain (DNMT1 D ) (Fig. F).

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Source Sci Signal 2010 3, ra80. Entinostat (MS-275) purchased from Selleck
Method Flow cytometric analyses, Western blot, MANOVA analyses, Tumor Volume Measurements
Cell Lines HAUSPKO cells
Concentrations 5/10 μM
Incubation Time 72 h
Results We treated wild-type and HAUSP knockout cells with HDAC inhibitor MS-275, which induced 5 to 10 times as many apoptotic cells in HAUSP knockout cells relative to wild-type cells (Fig. A). Furthermore, HDAC inhibition increased the number of apoptotic cells (sub-G 1 cells) (Fig. B) and increased the abundance of apoptotic cell markers including cleaved caspases 3, 6, and 9, and poly(adenosine diphosphate-ribose) polymerase (PARP) (Fig. C). Furthermore, degradation of DNMT1 was the major cause of cell death, because ectopic overexpression of DNMT1 in the HAUSP knockout cells partially rescued HDAC inhibitor-induced apoptosis (Fig. D). Moreover, HAUSP knockout cells were more sensitive to growth arrest caused by MS-275 (Fig. E)when grown in cell culture.

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Source J Am Heart Assoc 2012 1, e000901. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines human aortic SMCs
Concentrations
Incubation Time
Results Both TSA and MS-275 significantly suppressed the induction of S MC proteins by Notch activation.

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Source Breast Cancer Res Treat 2012 131, 777-789. Entinostat (MS-275) purchased from Selleck
Method MTT growth inhibition and drug combination index (CI) analysis
Cell Lines MDA-MB-231 cells
Concentrations
Incubation Time 48 h
Results At very low dose combination (fractional growth inhibition,Fa=0.9), synergistic growth inhibition (CI<1) was observed between pargyline and HDAC inhibitors SAHA,TSA,MS-275, and LBH-589.At median or higher dose combination (Fa = 0.5 or 0.75), pargyline exhibited synergy with all the HDAC inhibitors tested (CI<1)

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Source Exp Dermatol 2010 19, 1096-1102. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cells, MDA-MB-468 cells
Concentrations 0.5-10 μM
Incubation Time 24 h
Results In both MDA-MB-231 and MDA-MB-468 cell lines, exposure to MS-275 and other compounds produced significant global increase of nuclear H3K4me2,which is the specific substrate of LSD1.The enhanced level of histone methylation by HDAC inhibitors parallels the increase of acetylation of histone 3

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Source Mol Pain 2010 6, 51. Entinostat (MS-275) purchased from Selleck
Method Immunoblot, Immunofluorescent histochemistry
Cell Lines lumbar spinal cord
Concentrations 0.5 μg
Incubation Time 30 min
Results As shown in Fig. A and B, the relative H3K9 acsignals in animals injected either with SAHA or with MS-275 were largely enhanced in comparison to that in animals receiving i.t. saline. Using an antibody specific to acety-lated H3 lysine 9/18 (H3K9/18ac) for immunohisto-chemistry, we further observed that 30 min after the injection, the signals of H3K9 /18ac robustly increased in the lumbar spinal cord (Fi g. C)

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Source PLoS One 2013 8, e74930. Entinostat (MS-275) purchased from Selleck
Method Western blot, real-time PCR
Cell Lines Human dermal fibroblasts
Concentrations 1 uM
Incubation Time 48 h
Results blockade of HDAC1 by entinostat significantly increased mRNA and protein levels of the type I collagen gene

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Source Biochem Bioph Res Co 2010 414, 25-30. Entinostat (MS-275) purchased from Selleck
Method qRT-PCR
Cell Lines HEK-293cells
Concentrations 0.37-10uM
Incubation Time
Results Analysis of mRNA changes following MS-275 treatment revealed a different profile than what was observed with the paninhibitors. Class I specific HDAC inhibition increased both total and exon 7 included mRNA. However, the fold increases of the total transcript exceeded that of exon 7 included.

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Source Biochem Biophys Res Commun 2014 10.1016/j.bbrc.2014.01.184. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines HCT116 p54 null cells
Concentrations 1 uM
Incubation Time 24 h
Results MS-275 causes ER stress and increase the expression of ATF4, ATF3, CHOP.

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Source Biochem Biophys Res Commun 2014 10.1016/j.bbrc.2014.01.184. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines HCT116 p53 null cells
Concentrations 1 uM
Incubation Time 24 h
Results Knockdown of ATF3 suppressed the induction of DR5 protein and knockdown of ATF4 suppressed the induction of ATF3, CHOP and DR5 proteins by these HDACIs(TSA, M344, MS-275).

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Source 2011 Dr. Zhang of Tianjin Medical University. Entinostat (MS-275) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cells
Concentrations 0-20 μM
Incubation Time
Results Western blot analysis of Acetyl-H3 and H3. 0-20μM MS-275 was added.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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