1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. HDAC
    Autophagy
    Mitophagy
  3. Vorinostat

Vorinostat (Synonyms: SAHA)

Cat. No.: HY-10221 Purity: 99.90%
Handling Instructions

Vorinostat is a potent and orally available inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.

For research use only. We do not sell to patients.

Vorinostat Chemical Structure

Vorinostat Chemical Structure

CAS No. : 149647-78-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
250 mg USD 60 In-stock
Estimated Time of Arrival: December 31
500 mg USD 102 In-stock
Estimated Time of Arrival: December 31
1 g USD 120 In-stock
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5 g USD 420 In-stock
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Customer Review

Based on 28 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Vorinostat purchased from MCE. Usage Cited in: Mol Psychiatry. 2017 May;22(5):711-723.

    Oral SAHA administration increases brain plasma membrane calcium ATPase (PMCA) levels, reduces oxidative stress, improves behavioral deficits and prevents neurodegeneration in ASM knockout (ASMko) mice. (a,b) Western blot of hippocampal membrane extracts from wt (a) and ASMko (b) mice orally administered SAHA complexed to HOP-β-CDX (SAHA) or HOP-β-CDX (control), and probed for PMCA and ATP6V1A.

    Vorinostat purchased from MCE. Usage Cited in: Oncotarget. 2017 May 23;8(21):34362-34373.

    Notch3 protein levels after treatment with SAHA at different concentrations or DMSO (vehicle control), determined by western blot.

    Vorinostat purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753.

    Synergistic Decrease Bcl-2 Expression by the Combination of Vorinostat with Dasatinib in MCF-7 Cells.

    Vorinostat purchased from MCE. Usage Cited in: Nat Commun. 2017 Dec 20;8(1):2207.

    HCT116 cells are treated with Vorinostat for 24 h, followed by by western blot analysis for the indicated proteins.

    Vorinostat purchased from MCE. Usage Cited in: RSC Adv., 2018, 8, 17279-17292

    The NH2 cells expressing Tat. All tested cells are treated with SAHA for 24 h. The expression of GFP for tested J-Lat A2 and 2D10 cells is measured by FACS. Whole cell extracts for tested NH1 and NH2 cells are prepared and examined for the luciferase activities.

    Vorinostat purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 May 18. pii: S1874-9399(18)30028-2.

    Jurkat T cells are treated for various times with Vorinostat 1 μM and Chidamide at 0.6 μM. Levels of SALL2 and cleaved PARP are evaluated by Western blot analysis. β-actin is used as a loading control.

    Vorinostat purchased from MCE. Usage Cited in: Universidad Autónoma de Madrid, Facultad de Ciencias, Departamento de Biología Molecular. 15-06-2015.

    SAHA, a histone deacetylase inhibitor that is shown to increase PMCA levels and to enhance calcium clearance in a breast cancer cell model.
    • Biological Activity

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    Description

    Vorinostat is a potent and orally available inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.

    IC50 & Target

    ID50: 10 nM (HDAC1), 20 nM (HDAC3)[3]
    HDAC2, HDAC7[1], HDAC11[4]

    In Vitro

    Vorinostat efficiently suppresses MES-SA cell growth at a low dosage (3 μM) already after 24 hours treatment. HDACs class I (HDAC2 and 3) as well as class II (HDAC7) are preferentially affected by this treatment. Vorinostat significantly increases p21WAF1 expression and apoptosis in MES-SA cells[1]. Vorinostat inhibits SK-N-SH and SK-N-Be(2)C with the IC25 values of 1 µM and 0.5 µM, respectively[2].

    In Vivo

    Vorinostat (50 mg/kg/day) reduces tumor growth by more than 50% in nude mice injected with 5×106 MES-SA cells[1].

    Clinical Trial
    Molecular Weight

    264.32

    Formula

    C₁₄H₂₀N₂O₃

    CAS No.

    149647-78-9

    SMILES

    O=C(NC1=CC=CC=C1)CCCCCCC(NO)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (378.33 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7833 mL 18.9165 mL 37.8329 mL
    5 mM 0.7567 mL 3.7833 mL 7.5666 mL
    10 mM 0.3783 mL 1.8916 mL 3.7833 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (9.46 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (9.46 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.46 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Cell lysates are prepared by using RIPA buffer (25 mM Tris-HCl pH 7.6, 150 mM NaCl, 1% NP-40, 1% sodium deoxycholate, 0.1% SDS), and the protein concentration is determined by Bio-Rad DC Protein Assay. Protein lysates are separated by SDS-PAGE and transferred to nitrocellulose membrane. Following antibodies and dilutions are used: rabbit anti HDAC1 (1 μg/mL); rabbit anti HDAC2 (1 μg/mL); rabbit anti HDAC3 (9 μg/mL); rabbit anti HDAC7 (3 μg/mL); mouse anti p21WAF1 (0.5 μg/mL). As secondary antibodies, the rabbit anti-mouse and swine anti-rabbit HRP-coupled antibodies at a final concentration of 1 μg/mL. An overnight incubation at 4°C is used for all primary antibodies, followed by washing and 2-hours incubation at RT with secondary antibodies. Specific protein bands are visualized by enhanced chemiluminescence assay. To demonstrate equal loading of protein samples all western blots are probed for β-tubulin.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Twelve weeks old male mice (n=14) are anesthetized with Isofluran and 5×106 MES-SA cells are injected subcutaneously into the right flank of the animal. Mice from a control group receives placebo containing 300 μL of empty HOP-β-CD (2-hydroxypropyl-β-cyclodextrin) vesicles. Another group of mice receives vorinostat dissolved in HOP-β-CD at a concentration of 50 mg/kg/day. Both, empty vesicles and vorinostat are administered intraperitoneally, starting on the day 4 after the injection of MES-SA tumor cells. Mice body weight and tumor size (w2 × l × 0.52; measured by caliper) are estimated twice a week. All mice are treated for 21 days and afterwards sacrificed by cervical dislocation. Each tumor is isolated as a whole and different tumor parameters are determined. Finally, tumor slices are cryo preserved and formalin fixed (4%) for further analyses.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.90%

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