| 规格或纯度 | ≥98% |
|---|---|
| 英文名称 | MG-132 (Ethanol Solution) |
| 生化机理 | 细胞渗透性强，可逆的蛋白酶体抑制剂（K i = 4 nM）。通过26S复合物减少哺乳动物细胞中泛素结合蛋白的降解，而不会影响其ATPase或异肽酶的活性。 |
| 储存温度 | -20°C储存,干燥 |
| 运输条件 | 超低温冰袋运输 |
| 备注 | 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 |
在室温下运输。储存在-20℃。存放在干燥的条件下。 Shipped at Room Temperature. Store at -20°C. Store under desiccating conditions. |
| IUPAC 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 | 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 |
| Canonical SMILES | CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 |
| 分子式 |
C26H41N3O5 |
| PubChem CID | 462382 |
| 分子量 | 475.62 |
| PubChem CID | 462382 |
|---|---|
| ChEMBL Ligand | CHEMBL64925 |
| CAS Registry No. | 133407-82-6 |
| RCSB PDB Ligand | LDZ |
| 溶解性 | Supplied in ethanol (10 mM) |
|---|
| Target ID | 2405 | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | proteasome 20S subunit beta 2 | ||||||||||||||||||||||||
| 缩写名 | SHP2 | ||||||||||||||||||||||||
| 家族 | T1: Proteasome | ||||||||||||||||||||||||
| 别名 | food intake receptor | ||||||||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||||||||
| OMIM | 602175 (Hs) | ||||||||||||||||||||||||
| Entrez Gene | 5690 (Hs) , 26445 (Mm) , 29675 (Rn) | ||||||||||||||||||||||||
| UniProtKB | P49721 (Hs) , Q9R1P3 (Mm) , P40307 (Rn) | ||||||||||||||||||||||||
| RefSeq Protein | NP_002785 (Hs) , NP_036100 (Mm) , NP_058980 (Rn) | ||||||||||||||||||||||||
| RefSeq Nucleotide | NM_002794 (Hs) , NM_011970 (Mm) , NM_017284 (Rn) | ||||||||||||||||||||||||
| Ensembl Gene | ENSG00000126067 (Hs) , ENSMUSG00000028837 (Mm) , ENSRNOG00000011463 (Rn) | ||||||||||||||||||||||||
| MEROPS | T01.984 (Hs) | ||||||||||||||||||||||||
| Protein GI | 4506195 (Hs) , 227116345 (Mm) , 8394079 (Rn) | ||||||||||||||||||||||||
| DrugBank Target | P49721 (Hs) | ||||||||||||||||||||||||
| CATH/Gene3D | 3.60.20.10 (N/A) | ||||||||||||||||||||||||
| ChEMBL Target | CHEMBL3492 (Hs) , CHEMBL3112378 (Mm) |
| Target ID | 2406 | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | proteasome 20S subunit beta 5 | ||||||||||||||||||||||||
| 缩写名 | SHP2 | ||||||||||||||||||||||||
| 家族 | T1: Proteasome | ||||||||||||||||||||||||
| 别名 | food intake receptor | ||||||||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||||||||
| OMIM | 600306 (Hs) | ||||||||||||||||||||||||
| Entrez Gene | 5693 (Hs) , 19173 (Mm) , 29425 (Rn) | ||||||||||||||||||||||||
| UniProtKB | P28074 (Hs) , O55234 (Mm) , P28075 (Rn) | ||||||||||||||||||||||||
| RefSeq Protein | NP_001124197 (Hs) , NP_001138404 (Hs) , NP_002788 (Hs) , NP_035316 (Mm) , NP_001099197 (Rn) | ||||||||||||||||||||||||
| RefSeq Nucleotide | NM_001130725 (Hs) , NM_001144932 (Hs) , NM_002797 (Hs) , NM_011186 (Mm) , NM_001105727 (Rn) | ||||||||||||||||||||||||
| Ensembl Gene | ENSG00000100804 (Hs) , ENSMUSG00000022193 (Mm) , ENSRNOG00000013386 (Rn) | ||||||||||||||||||||||||
| MEROPS | T01.P01 (Hs) | ||||||||||||||||||||||||
| Protein GI | 195539356 (Hs) , 222144262 (Hs) , 4506201 (Hs) , 6755204 (Mm) , 160333293 (Rn) | ||||||||||||||||||||||||
| DrugBank Target | P28074 (Hs) | ||||||||||||||||||||||||
| CATH/Gene3D | 3.60.20.10 (N/A) | ||||||||||||||||||||||||
| ChEMBL Target | CHEMBL4662 (Hs) , CHEMBL4523208 (Rn) , CHEMBL1944494 (Mm) |
| Target ID | 3111 | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | CoV 3C-like (main) protease | ||||||||||||||||||
| 缩写名 | SHP2 | ||||||||||||||||||
| 家族 | Coronavirus (CoV) proteins | ||||||||||||||||||
| 别名 | MB-IRK3 | ||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||
| RefSeq Protein | YP_009725301 (SARS-CoV-2) | ||||||||||||||||||
| UniProtKB | P0C6U8 (SARS-CoV) | ||||||||||||||||||
| ChEMBL Target | CHEMBL3927 (SARS-CoV) |
| Ligand ID | 8616 |
|---|---|
| 名称 | MG-132 |
| 别名 | MG132 |
| 类别 | Peptide |
| 学名 | phenylmethyl 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 |
| 生物活性评价 |
Compound 5b also inhibits cathepsin B activity with a Ki of 12nM. In vitro, compound 5b inhibits growth of human prostate PC3 tumour cells |
| 评价 |
Compound 5b is reported to inhibit the enzymatic activity of proteasome macropain |
| 单字母多肽序列 | LLL |
| 三字母多肽序列 | Z-Leu-leu-leu-al |
| 翻译后修饰 | |
| 化学修饰 |
| 1. Rydzewski RM, Burrill L, Mendonca R, Palmer JT, Rice M, Tahilramani R, Bass KE, Leung L, Gjerstad E, Janc JW et al.. (2006) Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.. J Med Chem, 49 (10): (2953-68). [PMID:16686537] |
| 2. Chen W et al.. (2021) MARCH8 Suppresses Tumor Metastasis and Mediates Degradation of STAT3 and CD44 in Breast Cancer Cells.. Cancers (Basel), 13 (11): (). [PMID:34067416] |
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