1. Metabolic Enzyme/Protease
    NF-κB
    Apoptosis
    Autophagy
  2. Proteasome
    NF-κB
    Apoptosis
    Autophagy
  3. Bortezomib

Bortezomib (Synonyms: 硼替佐米; PS-341; LDP-341; NSC 681239)

目录号: HY-10227 纯度: 99.95%
产品使用指南

Bortezomib (PS-341) 是一种可逆性和选择性的蛋白酶体 (proteasome) 抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一种蛋白酶体抑制剂,具有抗癌活性。

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Bortezomib Chemical Structure

Bortezomib Chemical Structure

CAS No. : 179324-69-7

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10 mM * 1 mL in DMSO ¥561 In-stock
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10 mg ¥660 In-stock
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Customer Review

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

    Bortezomib purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.

    Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Bortezomib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.

    AGS cells are pretreated with 25 and 50 nM Bortezomib for 1 h, and then incubated with 500 nM Torin 1 for 24 h. After pretreatment with PPI for 24 h in pH 7.4 or pH 6.5 condition, Rapamycin (1 μM) or Torin 1 (500 nM) is added for another 24 h. The protein level of SQSTM1 is measured by western blot analysis.

    Bortezomib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.

    Different concentrations of two classical proteasome inhibitors Bortezomib and MG132 are added. AGS cells are either untreated or treated with Bortezomib (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

    Bortezomib purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Nov 15;815:147-155.

    Shown are GFPu fluorescent images of the GFPu-HEK293 cells treated with CuSO4 (Cu, 20 μM), HK (20 μM), HK-Cu (HC, 20 μM), or Velcade (Vel, 100 nM).

    Bortezomib purchased from MCE. Usage Cited in: BMC Cancer. 2018 Oct 11;18(1):971.

    The reduction of MAGEC2 protein level in TRIM28-knockdown A375 cells can be inhibited by treatment with both MG132 and PS-341, and similar result is also observed in Hs 695 T cells.

    Bortezomib purchased from MCE. Usage Cited in: Clin Cancer Res. 2019 Jun 15;25(12):3630-3642.

    H1975 cells treated with 5 μmol/L MTI-31 alone or in combination with 10 μmol/L CQ or 0.01 μmol/L PS-341.

    查看 NF-κB 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

    IC50 & Target

    Ki: 0.6 nM (20S proteasome)[1]

    体外研究
    (In Vitro)

    Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1[1].
    Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines[3].
    Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines[3].
    The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells[4].
    Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3)[5].

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

    Cell Cycle Analysis[1]

    Cell Line: PC-3 cells
    Concentration: 100 nM
    Incubation Time: 8 hours
    Result: Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.

    Apoptosis Analysis[3]

    Cell Line: JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
    Concentration: 5-100 nM
    Incubation Time: 20 hours
    Result: The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).

    Western Blot Analysis[3]

    Cell Line: wtp53 (Granta-519), mutp53 (Jeko) cells
    Concentration: 20 nM
    Incubation Time: 1, 2, 4, 6, 14 hours
    Result: Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).
    体内研究
    (In Vivo)

    Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice[1].

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

    Animal Model: Male nude mice (xenograft tumor model bearing PC-3 cells)[1]
    Dosage: 0.3, 1 mg/kg
    Administration: Intravenous injection; once weekly for 4 weeks
    Result: Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.
    Clinical Trial
    分子量

    384.24

    Formula

    C₁₉H₂₅BN₄O₄

    CAS 号
    中文名称
    SMILES

    OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (260.25 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6025 mL 13.0127 mL 26.0254 mL
    5 mM 0.5205 mL 2.6025 mL 5.2051 mL
    10 mM 0.2603 mL 1.3013 mL 2.6025 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 (protect from light)。-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: 1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.41 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
    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.41 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
    • 4.

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

      Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (5.41 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。

    • 5.

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

      Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution

    • 6.

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

      Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    Purity: 99.97%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    BortezomibPS-341 LDP-341 NSC 681239PS341PS 341LDP341LDP 341LDP-341NSC681239NSC 681239NSC-681239ProteasomeNF-κBApoptosisAutophagyNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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    目录号:
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