HMB-Val-Ser-Leu-VE |
Catalog No.GC16699
One-Click Copy Product Info
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inhibitor of the trypsin-like activity of the 20S proteasome
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 862891-04-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 862891-04-1 | SDF | |
| 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 | ||
| Formula | C26H39N3O7 | M.Wt | 505.6 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9778 mL | 9.8892 mL | 19.7785 mL |
| 5 mM | 395.6 μL | 1.9778 mL | 3.9557 mL |
| 10 mM | 197.8 μL | 988.9 μL | 1.9778 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)