2. Cell Cycle/DNA Damage Epigenetics Autophagy Anti-infection Apoptosis
  3. HDAC Autophagy Mitophagy Filovirus Apoptosis HPV
  4. Vorinostat

Vorinostat  (Synonyms: SAHA; Suberoylanilide hydroxamic acid)

Cat. No.: HY-10221 Purity: 99.62%
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Vorinostat (SAHA) est un pan-inhibiteur puissant et oralement actif des HDAC1, HDAC2 et HDAC3 (classe I), HDAC7 ( Classe II) et HDAC11 (Classe IV), avec des valeurs ID50 de 10 nM et 20 nM pour HDAC1 et HDAC3, respectivement. Vorinostat induit l'apoptose cellulaire.

Vorinostat (SAHA) ist ein potenter und oral wirksamer Pan-Inhibitor von HDAC1, HDAC2 und HDAC3 (Class I), HDAC7 (Class II) und HDAC11 (Class IV), mit ID50-Werten von 10 nM bzw. 20 nM für HDAC1 und HDAC3. Der Vorinostat induziert die apoptosis.

Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.

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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Customer Review

Based on 109 publication(s) in Google Scholar

Other Forms of Vorinostat:

Vorinostat Related Antibodies

Top Publications Citing Use of Products

102 Publications Citing Use of MCE Vorinostat

WB

    Vorinostat purchased from MedChemExpress. 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 MedChemExpress. Usage Cited in: Biochim Biophys Acta Gene Regul Mech. 2018 May 18;S1874-9399(18)30028-2.  [Abstract]

    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 MedChemExpress. Usage Cited in: Nat Commun. 2017 Dec 20;8(1):2207.  [Abstract]

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

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

    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 MedChemExpress. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753.  [Abstract]

    Synergistic Decrease Bcl-2 Expression by the Combination of Vorinostat with BMS-354825 in MCF-7 Cells.

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

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

    Vorinostat purchased from MedChemExpress. 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.

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    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis[1][4]. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification[7].

    IC50 & Target[1][3][4]

    HDAC1

    10 nM (ID50)

    HDAC3

    20 nM (ID50)

    HDAC2

     

    HDAC7

     

    HDAC11

     

    Autophagy

     

    Mitophagy

     

    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].
    Vorinostat is an effective inhibitor of HPV-18 DNA amplification, reduces oncoproteins E6 and E7 activities and triggers apoptosis in HPV-infected, differentiated cells[7].

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

    Vorinostat Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    264.32

    Formula

    C14H20N2O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (378.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

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

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

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

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 3.33 mg/mL (12.60 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    COA (243 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7833 mL 18.9165 mL 37.8329 mL 94.5823 mL
    5 mM 0.7567 mL 3.7833 mL 7.5666 mL 18.9165 mL
    10 mM 0.3783 mL 1.8916 mL 3.7833 mL 9.4582 mL
    15 mM 0.2522 mL 1.2611 mL 2.5222 mL 6.3055 mL
    20 mM 0.1892 mL 0.9458 mL 1.8916 mL 4.7291 mL
    25 mM 0.1513 mL 0.7567 mL 1.5133 mL 3.7833 mL
    30 mM 0.1261 mL 0.6305 mL 1.2611 mL 3.1527 mL
    40 mM 0.0946 mL 0.4729 mL 0.9458 mL 2.3646 mL
    50 mM 0.0757 mL 0.3783 mL 0.7567 mL 1.8916 mL
    60 mM 0.0631 mL 0.3153 mL 0.6305 mL 1.5764 mL
    80 mM 0.0473 mL 0.2365 mL 0.4729 mL 1.1823 mL
    100 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
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    Vorinostat Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vorinostat149647-78-9SAHA Suberoylanilide hydroxamic acidHDACAutophagyMitophagyFilovirusApoptosisHPVHistone deacetylasesMitochondrial AutophagyHuman papillomavirusInhibitorinhibitorinhibit

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