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

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

目录号: HY-10227G
产品使用指南 技术支持

Bortezomib (GMP) (PS-341 (GMP)) 是 GMP 级别的 Bortezomib (HY-10227)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。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

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Bortezomib 的其他形式现货产品:

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Other Forms of Bortezomib:

Bortezomib 相关抗体

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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].

体外研究
(In Vitro)

Bortezomib (GMP) (PS-341 (GMP)) (100 nM；8 小时) 导致 G2-M 期细胞积累，G1 期细胞数量相应减少[1]。
Bortezomib (GMP) (5-100 nM；20 小时) 在套细胞淋巴瘤 (MCL) 细胞系中诱导细胞凋亡[3]。
Bortezomib (GMP) (20 nM；1-14 小时) 在两种 MCL 细胞系[3]中诱导 Noxa 上调。
Bortezomib (GMP) 的 IC50 是发现 B16F10 细胞中 26S 蛋白酶体的浓度为 2.46 nM[4]。
Bortezomib (GMP) 抑制多种抗凋亡蛋白 (例如，Bcl-XL、Bcl-2、和 STAT-3)[5]。 JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)[3] 5-100 nM 20 hours The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM). wtp53 (Granta-519), mutp53 (Jeko) cells[3] 20 nM 1, 2, 4, 6, 14 hours Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).

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

Bortezomib 相关抗体:

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.

Cell Viability Assay[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 (GMP) (PS-341 (GMP)) (0.3-1 mg/kg；静脉注射；每周一次，持续 4 周) 抑制裸鼠体内的 PC-3 肿瘤生长[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.
分子量

384.24

Formula

C19H25BN4O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Bortezomib 相关分类

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  • 稀释计算器

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

Bortezomib (GMP)PS-341 (GMP)LDP-341 (GMP)NSC 681239 (GMP)ProteasomeNF-κBApoptosisAutophagyNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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