硼替佐米

Name: 硼替佐米
Brand: MM

≥98% (LC/MS), solid, 20S proteasome inhibitor, Calbiochem^®

别名:

硼替佐米, (R)-3-甲基-1-((S)-3-苯基-2-(吡嗪-2-羧酰胺基)丙酰胺基)丁基硼酸，BTZ，LDP-341，LDP341，MG341，MLN-341，MLN341，PS341，蛋白酶体抑制剂XXII，PS-341，MG-341，Pyz-Phe-boroLeu

登录查看公司和协议定价

选择尺寸

关于此项目

经验公式（希尔记法）:

C₁₉H₂₅BN₄O₄

化学文摘社编号:

179324-69-7

分子量:

384.24

MDL编号:

MFCD09056737

UNSPSC代码:

12352200

NACRES:

NA.77

主要文件

查看所有文档

技术服务

需要帮助？我们经验丰富的科学家团队随时乐意为您服务。

让我们为您提供帮助

技术服务

需要帮助？我们经验丰富的科学家团队随时乐意为您服务。

让我们为您提供帮助

产品名称

硼替佐米,

方案

≥98% (LC/MS)

质量水平

100

表单

solid

制造商/商品名称

Calbiochem^®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

颜色

off-white

溶解性

DMSO: 100 mg/mL
ethanol: 2 mg/mL (with sonication)

储存温度

−20°C

SMILES字符串

B(O)(O)[C@@H](NC(=O)[C@@H](NC(=O)c2nccnc2)Cc1ccccc1)CC(C)C

InChI

1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1

InChI key

GXJABQQUPOEUTA-RDJZCZTQSA-N

正在寻找类似产品? 访问产品对比指南

一般描述

硼替佐米是一种细胞渗透性的二肽基硼酸酯化合物，用作蛋白酶体抑制剂。蛋白酶体系统在细胞蛋白周转中发挥重要作用，对于细胞稳态维持至关重要。硼替佐米可逆结合26S蛋白酶体的胰凝乳蛋白酶样亚基抑制其功能，从而抑制多个促凋亡因子的降解。硼替佐米选择性抑制20S蛋白酶体β5 ChTL/胰凝乳蛋白酶样活性、β1 Cl/胱天蛋白酶样活性和β2 TL/胰蛋白酶样活性（各自的kinact/Ki = 38,000、5,700、<100 M-1s-1，人体20S蛋白酶体检测使用10 M Suc-LLVY-AMC/货号539142，10M Z-LLE-AMC/货号539141，或50M Boc-LRR-AMC作为底物；1小时内各自IC50 = 7, 74和4,200 nM），通过催化β亚基的亲核Thr1羟基/Thr10γ与抑制剂亲电子硼部分之间以一种共价、缓慢可逆方式相互作用而进行抑制，对人胰凝乳蛋白酶、组织蛋白酶G、白细胞弹性蛋白酶和凝血酶展现出的效力大大降低（各自Ki = 0.32, 0.63, 2.3和13 M，对比使用620 nM兔肌肉20S）。一种在体外培养和动物体内中广泛使用的抑制剂。尽管是首个被FDA批准用于临床抗癌治疗的蛋白酶体抑制剂，它的治疗功效仍然受到了脱靶作用和剂量限制性毒性的影响。

应用

硼替佐米已用于诱发小鼠的有氧糖酵解/神经病理性疼痛，研究化疗所致痛性周围神经病变。

生化/生理作用

可逆性：是

细胞可渗透性：具有

特点和优势

细胞可渗透，可靶向作用
可逆调节细胞过程

包装

用惰性气体包装

制备说明

仅使用新鲜的DMSO或乙醇用于重悬。

在重悬后分装并冻存于冰箱（-20°C.）储备溶液在-20°C下可稳定保存至多6个月。

其他说明

Du, X.L, and Chen, Q. 2013.Acta Haematol.129, 207.
Tamatani, T., et al. 2013.Int. J. Oncol.42, 935.
Beck, P., et al. 2012.J. Biol. Chem.393, 1101.
Fang, H.T., et al. 2012.Proc.Natl.Acad.Sci. USA.109, 2521.
Chen, D., et al. 2011.Curr.Cancer Drug Targets11, 239.
Demo, S.D., et al. 2007.Cancer Res.67, 6383.
Adams, J., et al. 1999.Cancer Res.59, 2615.
Teicher, B.A., et al. 1999.Cancer Res.5, 2638.
Adams, J., et al. 1998.Bioorg.Med. Chem. Lett.8, 333.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

毒性：标准处理（A）

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

输入产品批号来搜索分析证书(COA) 。批号可以在产品标签上"批“ （Lot或Batch）字后找到。

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

Targeting metabolic pathways alleviates bortezomib-induced neuropathic pain without compromising anticancer efficacy in a sex-specific manner.

Panjamurthy Kuppusamy et al.

Frontiers in pain research (Lausanne, Switzerland), 5, 1424348-1424348 (2024-07-09)

Chemotherapy-induced peripheral neuropathy (CIPN) is a debilitating side effect of cancer treatment that significantly impacts patients' quality of life. This study investigated the effects of targeting metabolic pathways on bortezomib-induced neuropathic pain and tumor growth using a Lewis lung carcinoma

Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome.

Susan D Demo et al.

Cancer research, 67(13), 6383-6391 (2007-07-10)

Clinical studies with bortezomib have validated the proteasome as a therapeutic target for the treatment of multiple myeloma and non-Hodgkin's lymphoma. However, significant toxicities have restricted the intensity of bortezomib dosing. Here we describe the antitumor activity of PR-171, a

Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

J Adams et al.

Bioorganic & medicinal chemistry letters, 8(4), 333-338 (1999-01-01)

Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.

The proteasome inhibitor PS-341 in cancer therapy.

B A Teicher et al.

Clinical cancer research : an official journal of the American Association for Cancer Research, 5(9), 2638-2645 (1999-09-28)

The anticancer activity of the boronic acid dipeptide proteasome inhibitor PS-341 was examined in vitro and in vivo. PS-341 was a potent cytotoxic agent toward MCF-7 human breast carcinoma cells in culture, producing an IC90 of 0.05 microM on 24

Bortezomib interferes with C-KIT processing and transforms the t(8;21)-generated fusion proteins into tumor-suppressing fragments in leukemia cells.

Hai-Tong Fang et al.

Proceedings of the National Academy of Sciences of the United States of America, 109(7), 2521-2526 (2012-02-07)

The boronic acid dipeptide bortezomib inhibits the chymotrypsin-like activity of the 26S proteasome and shows significant therapeutic efficacy in multiple myeloma. However, recent studies suggest that bortezomib may have more complex mechanisms of action in treating cancer. We report here

查看所有相关文献

硼替佐米

≥98% (LC/MS), solid, 20S proteasome inhibitor, Calbiochem®

选择尺寸

关于此项目

主要文件

属性

产品名称

方案

质量水平

表单

制造商/商品名称

储存条件

颜色

溶解性

储存温度

SMILES字符串

InChI

InChI key

相关类别

说明

一般描述

应用

生化/生理作用

特点和优势

包装

制备说明

其他说明

法律信息

免责声明

安全信息

储存分类代码

WGK

闪点(°F)

闪点(°C)

文件

分析证书(COA)

已有该产品？

同行评审论文

技术文章和实验方案

相关内容

技术服务

≥98% (LC/MS), solid, 20S proteasome inhibitor, Calbiochem^®