Bortezomib (PS-341)

For research use only. Not for use in humans.

目录号：S1013 别名： LDP-341, MLM341 中文名称：硼替佐米

CAS No. 179324-69-7

Bortezomib (PS-341, LDP-341, MLM341)是有效的蛋白酶抑制剂，K_i为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib (PS-341) 可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。

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10mM (1mL in DMSO)	RMB 749.39	现货
5mg	RMB 571.94	现货
25mg	RMB 2188.92	现货
100mg	RMB 5488.32	现货
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客户使用Selleck生产的Bortezomib (PS-341)发表文献651篇：

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产品安全说明书

Proteasome抑制剂选择性比较

生物活性

产品描述

靶点

NF-κB ^[6] ()	20S proteasome ^[1] (Cell-free assay)
	0.6 nM(Ki)

体外研究

Bortezomib，一种硼酸二肽，是一种26S蛋白酶体的高选择性可逆抑制剂，其作用于错误折叠蛋白的降解，并且对细胞周期的调控是必要的。暴露于Bortezomib能够稳定p21，p27，和p53，以及促凋亡Bid和Bax蛋白，微囊蛋白-1，和抑制剂κB-α，这防止了核因子κB诱导的细胞存活途径的激活。Bortezomib也会促进促凋亡c-Jun-NH2末端激酶，以及内质网应激反应的激活。这些细胞蛋白水平的改变导致对增殖，迁移的抑制，和癌细胞凋亡的促进。^[2] Bortezomib能够渗透到细胞，并抑制蛋白酶体介导的细胞内长寿蛋白水解，抑制50%蛋白质水解的浓度为∼0.1 μM。Bortezomib对衍生自美国国家癌症研究所(NCI)多重人类肿瘤的一组60个癌细胞系的IC50值为7 nM。PC-3细胞用Bortezomib (100 nM)处理8小时导致细胞积聚在G2-M期，相应的G1期细胞数量减少。Bortezomib在24和48小时杀死PC-3细胞，IC50分别为100和20 nM。Bortezomib治疗16-24小时后诱导细胞核缩合。Bortezomib在低至100 nM浓度下以时间依赖的方式导致PARP裂解，在处理24小时后产生效果。^[1]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
NCI-H1838	NIjleZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{W0TGlEPTB;NEG4Ok4{OiEQvF2=	MnnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN\|I2ODRzLze+V2FPT0WUPD;hQi=>
IMR-5	MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mk\rTWM2OD1\|NEC5MlYzKM7:TR?=	NVOyZZc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
TE-441-T	NXjPSGxjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVHCfYNKUUN3ME2yOVIyNjdizszN	NXnTOIF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
U-698-M	MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1q3fmlEPTB;MkK2Nk4yPSEQvF2=	NFr4SFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK\|5USU6JRWK8M4E,
COLO-824	NV\0THlQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3L6e2lEPTB;MUK2NU44QCEQvF2=	M{DFS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
P31-FUJ	Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXu3VZN1UUN3ME2xNVEzNjd3IN88US=>	MlmxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN\|I2ODRzLze+V2FPT0WUPD;hQi=>
KY821	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{fPd2lEPTB;MUCzOk4xPCEQvF2=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzNlUxPDFxJ{7TRW5ITVJ:L3G+
RPMI-8866	NI\aV2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{nKUWlEPTB;MUCwOk4zQCEQvF2=	NWHWbGN3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
TC-YIK	NWjKTnlnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{\H[mlEPTB;N{ixMlAyKG6P	M1HmTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
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