1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. HDAC
    Autophagy

Entinostat (Synonyms: MS-275; SNDX-275)

Cat. No.: HY-12163 Purity: 98.29%
Data Sheet SDS Handling Instructions

Entinostat is the class I-selective HDAC inhibitor, with IC50 of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3.

For research use only. We do not sell to patients.
Entinostat Chemical Structure

Entinostat Chemical Structure

CAS No. : 209783-80-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $90 In-stock
100 mg $120 In-stock
200 mg $190 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

    Entinostat purchased from MCE. Usage Cited in: Carcinogenesis. 2015 Feb;36(2):192-201.

    Entinostat shows a mild inhibitory effect on cell growth.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Entinostat is the class I-selective HDAC inhibitor, with IC50 of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3.

    IC50 & Target

    IC50: 243 nM (HDAC1), 453 nM (HDAC2), 248 nM (HDAC3)[1]

    In Vitro

    Binding affinity of Entinostat (MS-275) against HDAC1 and HDAC2 is 282 nM and 156 nM, respectively[1]. Effects of the HDAC inhibitor Entinostat (MS-275) have been examined in human leukemia and lymphoma cells (U937, HL-60, K562, and Jurkat) as well as in primary acute myelogenous leukemia blasts in relation to differentiation and apoptosis. MS-275 displays dose-dependent effects in each of the cell lines. When administered at a low concentration (e.g., 1 μM), MS-275 exhibits potent antiproliferative activity, inducing p21CIP1/WAF1-mediated growth arrest and expression of differentiation markers (CD11b) in U937 cells. Entinostat (MS-275) potently induces cell death, triggering apoptosis in ~70% of cells at 48 h[2].

    In Vivo

    Entinostat (MS-27-275) at 49 mg/kg shows marked antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and a moderate effect against Capan-1 tumor. Entinostat at 24.5 mg/kg and 12.3 mg/kg also shows significant effects against these tumors. In addition, oral administration of Entinostat apparently increases the level of histone acetylation in HT-29 tumor xenografts 4-24 h after the administration[3]. MS-275 administration (3.5 mg/kg i.p.) to Experimental autoimmune neuritis (EAN) rats once daily from the appearance of first neurological signs greatly reduces the severity and duration of EAN and attenuated local accumulation of macrophages, T cells and B cells, anddemyelination of sciatic nerves. Further, significant reduction of mRNA levels of pro-inflammatory interleukin-1β, interferon-γ, interleukine-17, inducible nitric oxide synthaseand matrix metalloproteinase-9 is observed in sciatic nerves of MS-275 treated EAN rats. In addition, MS-275 treatment increases proportion of infiltrated Foxp3+ cells and anti-inflammatory M2 macrophages in sciatic nerves of EAN rats[4].

    Clinical Trial
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6567 mL 13.2834 mL 26.5668 mL
    5 mM 0.5313 mL 2.6567 mL 5.3134 mL
    10 mM 0.2657 mL 1.3283 mL 2.6567 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Biochemical assays of HDAC activity are carried out by Nanosyn in a reaction volume of 10 μL in 384-well microplates. A standard enzymatic reaction contains 5 μL of 2× HDAC inhibitor (e.g., Entinostat), 4 μL of 2.5× enzyme, and 1 μL of 10× substrate in assay buffer (100 mM HEPES, pH 7.5, 25 mM KCl, 0.1% BSA, 0.01% Triton X-100, 1% DMSO). Final concentration of all HDACs in the enzymatic assays is between 0.5 and 5 nM. A final substrate concentration of 1 μM FAM-RHKK(Ac)-NH2 or FAM-RHKK(trifluoroacetyl)-NH2 is used in all assays and found to be below the determined Km,app for each enzyme[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Entinostat (MS-275) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    SH-SY5Y cells are maintained under normal culture conditions in a humidified incubator at 37°C with 5% CO2 and are split twice weekly. Cells are plated in black 384-well plates at 2500 cells/well in 20-μL volume of DMEM/F-12 culture media supplemented with 10% FBS and permitted to adhere overnight. The following day, HDAC inhibitors (e.g., Entinostat) are serially diluted in 100% DMSO, and this series is subsequently cross-diluted into culture media. 5 μL of compound (e.g., Entinostat) diluted in media is added to the appropriate well of the cell plate to afford the indicated final concentration of inhibitor (e.g., Entinostat) with a final 0.1% DMSO. Treated cells are incubated under normal tissue culture conditions for 6, 24, 48, 72, or 96 h prior to quantitation of cellular ATP levels as measured using CellTiter-Glo reagents. Similarly, after 6 h of incubation with HDAC inhibitors (e.g., Entinostat), media from separate cell plates are aspirated, and cells are washed once with media containing no inhibitors. 25 μL of media supplemented with 10% FBS and 0.1% DMSO (no inhibitors) is added back to the cells, and cellular ATP levels are determined using CellTiter-Glo after 24, 48, 72, or 96 h of incubation. Luminescence is measured at each time point using an Envision Instrument with a 0.1 s count time[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Entinostat (MS-27-275) is dissolved in 0.05 N HCl, 0.1% Tween 80 (Mice)[3].
    Entinostat (MS-275) is suspended in PBS (Rat)[4].

    Mice[3]
    A2780 cells (9×106) are suspended in PBS and are injected subcutaneously into the flank of nude mouse. For the other tumor lines, KB-3-1, HCT-15, 4-1St, Calu-3, St-4, Capan-1, and HT-29, tumors are passaged several times before starting in vivo antitumor testing, and a tumor lump (2-3 mm in diameter) is transplanted subcutaneously into the flank of a nude mouse by using a trocar needle. Treatment (four or five mice in each experimental group) with the drugs is started after the tumors are confirmed to have grown in the body (tumor size, 20-100 mm3). Entinostat is administered orally once daily 5 days per week for 4 weeks. Tumor length and width are monitored twice weekly, and tumor volume is calculated.
    Rat[4]
    Male Lewis rats (8-10 weeks, 170-200 g) are housed under a 12-h light/dark cycle with free access to food and water. For therapeutic treatment, EAN rats receive i.p. injection of MS-275 (3.5 mg/kg) daily from day 10 to day 14 (six rats/group). For injection, MS-275 is suspended in phosphate buffered saline (PBS) and the same volume (1 mL) of PBS is given to control rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    376.41

    Formula

    C₂₁H₂₀N₄O₃

    CAS No.

    209783-80-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Entinostat
    Cat. No.:
    HY-12163
    Quantity: