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

Bortezomib (PS-341) Chemical Structure

CAS No. 179324-69-7

Bortezomib (PS-341, LDP-341, MLM341)是有效的蛋白酶抑制剂,Ki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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 749.39 现货
RMB 571.94 现货
RMB 2188.92 现货
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:

产品安全说明书

Proteasome抑制剂选择性比较

生物活性

产品描述 Bortezomib (PS-341, LDP-341, MLM341)是有效的蛋白酶抑制剂,Ki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。
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 Concentration Incubation Time Formulation 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>
MS-1 MmTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlW0TWM2OD15NUmuOFIhdk1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzNlUxPDFxJ{7TRW5ITVJ:L3G+
DMS-153 M{TjTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvDdXROUUN3ME23OFYvQDNibl2= MmHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|I2ODRzLze+V2FPT0WUPD;hQi=>
SUP-T1 NFm5WIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33XUmlEPTB;Nki2MlA1KG6P MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzNlUxPDFxJ{7TRW5ITVJ:L3G+
SCC-15 NH;TXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS2doxQUUN3ME22OlcvPDdibl2= M{HmV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
MSTO-211H NFT5[GlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\RTWM2OD13N{SuNlYhdk1? M1;UeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
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NCI-H889 NVnTfmxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHMfFh7UUN3ME20OlEvQTJibl2= MojmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|I2ODRzLze+V2FPT0WUPD;hQi=>
CPC-N Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjZ[2xKSzVyPUSwN{44PyCwTR?= M{P3RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
COLO-668 NGDHXpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYC3PIRQUUN3ME20NFMvPTdibl2= Mnr6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|I2ODRzLze+V2FPT0WUPD;hQi=>
NCI-H226 M2K0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\tVJlKSzVyPUSwN{4zOyCwTR?= M1m2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
TUR NEf5OZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN7Nj62NUBvVQ>? M2fRfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
DEL MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DRU2lEPTB;M{mxMlI4KG6P NYDlSFZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
NCI-H1963 NEXXUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLjSG5ZUUN3ME2zPFYvOTlibl2= NGnocY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
CA46 NELRVYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzWbpFKSzVyPUO3N{43OyCwTR?= NVfnT29oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
SNU-C1 NFSxVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHHNlhKSzVyPUO2Nk4xQSCwTR?= NWezNFBXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
THP-1 NYjR[YxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHyRlF3UUN3ME2zNlIvPiCwTR?= M{ToeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
SCH NV;Bb3g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\MeWlEPTB;M{KyMlIzKG6P NUfOXWtSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
NCI-H1522 NV[4cZc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNyNz6wOUBvVQ>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzNlUxPDFxJ{7TRW5ITVJ:L3G+
LNCaP-Clone-FGC Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzVdFBKSzVyPUK5OU4zPiCwTR?= NFG4UI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
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NCI-H187 MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJ6Nz6wPEBvVQ>? M1\ZSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
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KM-H2 M4jseGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;kTWM2OD1zOUeuNFUhdk1? M3jReVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
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