EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73262_C
泛素-蛋白酶体抑制剂；NF-κB通路抑制剂；IκB激活剂
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总览
(S)-MG132是一种可逆的、细胞渗透性蛋白酶体活性抑制剂(IC₅₀ = 100 nM；Kisselev & Goldberg)和钙蛋白酶（Calpain）的抑制剂 (IC₅₀= 1.2µM；Tsubuki等人)。泛素-蛋白酶体通路选择性地降解细胞内蛋白，从而清除受损或错误折叠的蛋白，并调节参与控制炎症过程和细胞周期调节的关键蛋白的可用性(S)-MG132 通过抑制 IκB 的降解来抑制NF-κB 的激活（IC₅₀ = 3 µM；Arlt 等人，Palombella 等人，Ortiz-Lazareno 等人）。
癌症研究
·阻断HeLa细胞DNA损伤引发的细胞凋亡（Zhang等人）。
·抑制NF-κB激活，使多种癌细胞对凋亡敏感（Arlt等人）。
·对多种人类癌细胞系的细胞毒性作用（Banerjee & Liefshitz）。
·抑制小鼠黑色素瘤（B16）和人眼部黑色素瘤（IPC227F）细胞系的生长（Vivier等人）。
细胞类型
癌细胞及细胞系
种属
人，小鼠，非人灵长类，其他物种，大鼠
研究领域
癌症
CAS 编号
133407-82-6
化学式
C₂₆H₄₁N₃O₅
纯度
≥98%
通路
NF-κB，泛素
靶点
IκB，蛋白酶体
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (2)
文献 (8)
Inhibition of NF-κB sensitizes human pancreatic carcinoma cells to apoptosis induced by etoposide (VP16) or doxorubicin
Oncogene 2001
Abstract
The transcription factor NF-kappaB has anti-apoptotic properties and may confer chemoresistance to cancer cells. Here,we describe human pancreatic carcinoma cell lines that differ in the responsiveness to the topoisomerase-2 inhibitors VP16 (20 microM) and doxorubicin (0.3 microM): Highly sensitive T3M4 [corrected] and PT45-P1 cells,and Capan-1 and A818-4 cells that were almost resistant to both anti cancer drugs. VP16,but not doxorubicin,transiently induced NF-kappaB activity in all cell lines,whereas basal NF-kappaB binding was nearly undetectable in T3M4 [corrected] and PT45-P1 cells,but rather high in Capan-1 and A818-4 cells,as demonstrated by gel-shift and luciferase assays. Treatment with various NF-kappaB inhibitors (Gliotoxin,MG132 and Sulfasalazine),or transfection with the IkappaBalpha super-repressor,strongly enhanced the apoptotic effects of VP16 or doxorubicin on resistant Capan-1 and 818-4 cells. Our results indicate that under certain conditions the resistance of pancreatic carcinoma cells to chemotherapy is due to their constitutive NF-kappaB activity rather than the transient induction of NF-kappaB by some anti-cancer drugs. Blockade of basal NF-kappaB activity by well established drugs efficiently reduces chemoresistance of pancreatic cancer cells and offers the potential for improved therapeutic strategies.
Proteasome inhibitors: from research tools to drug candidates.
Chemistry & biology 2001 AUG
Abstract
The 26S proteasome is a 2.4 MDa multifunctional ATP-dependent proteolytic complex,which degrades the majority of cellular polypeptides by an unusual enzyme mechanism. Several groups of proteasome inhibitors have been developed and are now widely used as research tools to study the role of the ubiquitin-proteasome pathway in various cellular processes,and two inhibitors are now in clinical trials for treatment of multiple cancers and stroke.
Potential of the proteasomal inhibitor MG-132 as an anticancer agent, alone and in combination.
Anticancer research 2001
Abstract
Proteasomal activity is required for normal cellular functions including cell division,where entry and exit from mitosis is strictly regulated by cyclins and cyclin-dependent kinases which are among the important substrates of the proteasomal degradative machinery. Inhibitors of proteasomal activity have been shown to be effective inducers of apoptosis in tumor cells and may be useful as anticancer agents,either alone or in combination with other drugs. We have examined the effect of MG-132,a dipeptide proteasomal inhibitor,on various human cancer cell lines. We have also examined the effect of MG-132 on normal CD34+ enriched primary human peripheral blood stem cells. Our results indicate that MG-312 is a potent anticancer agent with cytotoxic effects on a variety of human cancer cell lines irrespective of their p53 status. MG-132 was found to be more effective in combination with drugs such as doxorubicin and etoposide that act in the S/G2-phase of the cell cycle via a mechanism that involves stabilization of cyclin B1 and increased expression of Bax. Further,MG-132 inhibits CFU-GM colony formation of the CD34+ enriched PBSC population and this inhibition correlates with release of cyt C into the cytosol.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 133407-82-6 |
| Chemical Formula | C₂₆H₄₁N₃O₅ |
| 纯度 | ≥ 98% |
| Target | IκB, Proteasome |
| Pathway | NF-κB, Ubiquitin |
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