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MG-132,可逆蛋白酶体抑制剂

强大的可逆蛋白酶体抑制剂
32篇引用文献 COA COA
  • CAS编号: 133407-82-6
  • 分子式: C26H41N3O5
  • 分子量: 475.62
  • PubChem编号: 462382
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M126521-5mg
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M126521-50mg
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M126521-100mg
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M126521-250mg
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Amino Acid/Protein Metabolism (4559) Apoptosis (7108) Autophagy (2848) Metabolic Enzyme/Protease (4889) Proteasome (85)
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基本描述

别名 蛋白酶体抑制剂 | 碳苯并-L-亮氨酰-L-亮氨酰-L-亮氨酸
英文别名 MG132 | Z-LLL-CHO | KBio3_000059 | NCGC00161679-01 | s10322 | SMR002530629 | HMS1989B12 | n-benzyloxycarbonyl-l-leucyl-l-leucyl-l-leucinal | NCGC00161679-03 | NCGC00161679-04 | Z-Leu-leu-leucinal | KBioGR_000030 | {1-[1-(1-Formyl-3-methyl-butylcarbamoyl)-
规格或纯度 Moligand™, ≥98%
英文名称 MG-132
生化机理 MG-132 [Z-Leu-Leu-Leu-CHO]是一种蛋白酶体抑制剂，可用于干扰蛋白酶体调控的细胞内蛋白质降解。蛋白酶体处理的这些蛋白质参与了炎症过程和细胞周期调控，因此这类醛类蛋白酶体抑制剂具有广泛的相关性。MG-132 通过阻止 IκB 降解（IC50=3 μM）来抑制 NF-κB 激活（10 μM），从而阻止转录因子为癌细胞提供化疗抗性。它还是一种钙蛋白酶抑制剂。MG-132 [Z-Leu-Leu-Leu-CHO] 是 26S 蛋白酶体的抑制剂，也是 JNK1、c-Jun 和 c-Fos 的激活剂。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，这些产品最多可以使用一周。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

MG-132是一种蛋白酶体抑制剂，IC50为100 nM，也抑制钙蛋白酶，IC50为1.2 μM。A proteasome and NF-κB inhibitor.

氨基酸序列：Z-Leu-Leu-Leu-al

MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.
A proteasome and NF-κB inhibitor.
纯度 ≥98%

关联靶点（人）

PSMB5 Tclin 蛋白酶体亚基β5型(Proteasome subunit beta type-5) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
VDR Tclin Vitamin D receptor (26531 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CTSB Tchem Cathepsin B (3822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CTSK Tchem Cathepsin K (3011 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALDH1A1 Tchem Aldehyde dehydrogenase 1A1 (77053 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CTSS Tchem Cathepsin S (3285 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAPN2 Tchem Calpain 2 (185 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PSENEN Tchem Gamma-secretase subunit PEN-2 (38 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NFKBIA Tchem NF-kappaB inhibitor alpha (187 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDM2 Tchem p53-binding protein Mdm-2 (4545 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A498 (42825 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BT-474 (2113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
C8166 (1658 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CA46 (271 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Calu-6 (398 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CCRF-CEM (65223 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Daudi (625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DMS-79 (150 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EVSA-T (142 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HL-60 (67320 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Huh-7 (12904 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HuTu80 (255 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IM-9 (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAR (316 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JIYOYE (162 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
K562 (73714 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KM12 (47707 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MCF7 (126967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ML-2 (146 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MOLT-4 (49676 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NALM-6 (592 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H128 (54 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-H345 (89 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NCI-N87 (850 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NTERA-2-cl-D1 (234 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OVCAR-4 (44535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PSN1 (345 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Raji (5516 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RKO (1376 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPMI-8226 (44974 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RXF 393 (41971 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SCC-15 (194 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SF-126 (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-1 (285 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SK-MEL-2 (46422 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNU1 (253 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNU-16 (476 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SNU-5 (270 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SUP-T1 (191 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

CTSL Cathepsin L (58 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Schistosoma mansoni (6170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-12 (7051 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAW264.7 (28094 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRE7 Proteasome component C5 (37 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Vero C1008 (1716 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
vif Virion infectivity factor (174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
INCHI 1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1
InChi Key TZYWCYJVHRLUCT-VABKMULXSA-N
Smiles CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
Isomeric SMILES CC(C)C[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCC1=CC=CC=C1
分子量 475.62
Reaxy-Rn 11627647
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11627647&ln=

化学和物理性质

溶解性 Soluble in DMSO (25 mg/ml), 100% ethanol (25 mg/ml), chloroform:methanol solution (95:5) (10 mg/ml), water (<1 mg/ml), and DMF (~25 mg/ml).
敏感性 对空气、热敏感
分子量 475.600 g/mol
XLogP3 4.800
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 5
可旋转键计数Rotatable Bond Count 15
精确质量Exact Mass 475.305 Da
单同位素质量Monoisotopic Mass 475.305 Da
拓扑极表面积Topological Polar Surface Area 114.000 Ų
重原子数Heavy Atom Count 34
形式电荷Formal Charge 0
复杂度Complexity 644.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 3
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

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批号(Lot Number) 证书类型 货号
I2517666 分析证书 M126521
I2517668 分析证书 M126521
I2517669 分析证书 M126521
I2517673 分析证书 M126521
J2215385 分析证书 M126521
D2526027 分析证书 M126521
G2311031 分析证书 M126521
G2311036 分析证书 M126521
L2420077 分析证书 M126521
J2215346 分析证书 M126521
J2215386 分析证书 M126521
J2215387 分析证书 M126521
J2215388 分析证书 M126521
G2431038 分析证书 M126521
A2206709 分析证书 M126521
A2206712 分析证书 M126521
A2206714 分析证书 M126521
G1915081 分析证书 M126521
A1908042 分析证书 M126521
E2410029 分析证书 M126521
I2208513 分析证书 M126521
I2208514 分析证书 M126521
A2423030 分析证书 M126521
H2409105 分析证书 M126521

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蛋白酶抑制剂
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引用文献

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