| CAS NO: | 862891-04-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 505.6 |
| Cas No. | 862891-04-1 |
| Formula | C26H39N3O7 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| Chemical Name | N-(3-hydroxy-2-methylbenzoyl)-L-valyl-N-[(1S,2E)-4-ethoxy-1-(2-methylpropyl)-4-oxo-2-butenyl]-L-serinamide |
| Canonical SMILES | OC1=CC=CC(C(N[C@@H](C(C)C)C(N[C@@H](CO)C(N[C@@H](CC(C)C)/C=C/C(OCC)=O)=O)=O)=O)=C1C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
HMB-Val-Ser-Leu-VE is an irreversible, cell-permeable, potent and specific inhibitor of the trypsin-like activity of the 20S proteasome with IC50 value of 33 nM [1].
The 20S proteasome is a 700 kDa, cylinder-shaped protease with multiple catalytic centers within the ubiquitin-proteasome pathway and plays an important role in the selective degradation of intracellular proteins. Proteasomes remove abnormal proteins and play an important role in cell-cycle progression and apoptosis [1][2].
HMB-Val-Ser-Leu-VE is a tripeptide-based compound bearing a C-terminal vinyl ester that acts as a potent and selective inhibitor of the trypsin-like activity of the 20S proteasome with IC50 value of 33 nM [1]. In two colon-carcinoma cell lines (COO115, HCT116), HMB-Val-Ser-Leu-VE was nontoxic and did not affect cell proliferation. In HLA-A2 positive lymphoblastoid cells, HMB-Val-Ser-Leu-VE caused a dose-dependent increase of CLG-specific killing, suggesting that HMB-Val-Ser-Leu-VE favored the generation and presentation of immunogenic peptides presented by MHC class I molecules [1].
References:
[1]. Marastoni M, Baldisserotto A, Cellini S, et al. Peptidyl vinyl ester derivatives: new class of selective inhibitors of proteasome trypsin-like activity. J Med Chem. 2005 Jul 28;48(15):5038-42.
[2]. DeMartino GN, Slaughter CA. The proteasome, a novel protease regulated by multiple mechanisms.
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