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HMB-Val-Ser-Leu-VE Sale

目录号 : GC16699

A vinyl ester tripeptide inhibitor of proteasome trypsin-like activity

HMB-Val-Ser-Leu-VE Chemical Structure

Cas No.:862891-04-1

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1mg
¥984.00
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5mg
¥4,409.00
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10mg
¥7,820.00
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25mg
¥17,099.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 862891-04-1 SDF
化学名 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
分子式 C26H39N3O7 分子量 505.6
溶解度 ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9778 mL 9.8892 mL 19.7785 mL
5 mM 0.3956 mL 1.9778 mL 3.9557 mL
10 mM 0.1978 mL 0.9889 mL 1.9778 mL
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