推荐产品
产品名称
硼替佐米,
方案
≥98% (LC/MS)
质量水平
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
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
警告
毒性：标准处理（A）
制备说明
仅使用新鲜的DMSO或乙醇用于重悬。
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.
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
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
其他客户在看
D Chen et al.
Current cancer drug targets, 11(3), 239-253 (2011-01-21)
Targeting the ubiquitin-proteasome pathway has emerged as a rational approach in the treatment of human cancer. Based on positive preclinical and clinical studies, bortezomib was subsequently approved for the clinical use as a front-line treatment for newly diagnosed multiple myeloma
J Adams et al.
Cancer research, 59(11), 2615-2622 (1999-06-11)
The ubiquitin-proteasome pathway plays a critical role in the regulated degradation of proteins involved in cell cycle control and tumor growth. Dysregulating the degradation of such proteins should have profound effects on tumor growth and cause cells to undergo apoptosis.
Philipp Beck et al.
Biological chemistry, 393(10), 1101-1120 (2012-10-24)
The 20S proteasome core particle (CP) is the proteolytically active key element of the ubiquitin proteasome system that directs the majority of intracellular protein degradation in eukaryotic cells. Over the past decade, the CP has emerged as an anticancer therapy
Tetsuya Tamatani et al.
International journal of oncology, 42(3), 935-944 (2013-01-24)
Oral cancer cells have a significantly augmented nuclear factor-κB (NF-κB) activity and the inhibition of this activity suppresses tumor growth. Bortezomib is a proteasome inhibitor and a drug used for molecular-targeted therapy (targets NF-κB). In this study, we investigated whether
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
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