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

Vorinostat (Synonyms: 伏立诺他; SAHA; Suberoylanilide hydroxamic acid)

目录号: HY-10221 纯度: 99.58%
产品使用指南

Vorinostat (SAHA) 是一种有效的,可口服的 HDAC1HDAC2HDAC3 (Class I)HDAC6HDAC7 (Class II)Class IV (HDAC11) 的抑制剂,对 HDAC1/3 的 ID50 值分别为 10 nM 和 20 nM。Vorinostat 可以诱导细胞凋亡 (apoptosis)。Vorinostat 还是一种人类乳头瘤病毒 (HPV)-18 DNA 扩增的有效抑制剂。

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Vorinostat Chemical Structure

Vorinostat Chemical Structure

CAS No. : 149647-78-9

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 63 篇科研文献

    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 BMS-354825 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 Gene Regul Mech. 2018 May 18;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.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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

     

    体外研究
    (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].

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

    体内研究
    (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].

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

    Clinical Trial
    分子量

    264.32

    Formula

    C14H20N2O3

    CAS 号
    中文名称

    伏瑞斯特;伏立诺他

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 100 mg/mL (378.33 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 20% HP-β-CD in saline

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

    • 2.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

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

    • 3.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

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

    • 4.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 5.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 6.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 7.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 8.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 9.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (7.87 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (7.87 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    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.

    参考文献

    纯度: 99.90%

    • 摩尔计算器

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    × = ×
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