Z-VRPR-FMK
Based on 1 Customer Validation
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1381885-28-4
- Formula: C31H49FN10O6
- Molecular Weight:676.78
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| OCI-Ly3 | GI50 |
8.22 μM
Compound: Z-VRPR-fmk
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Antiproliferative activity against human OCI-LY3 cells assessed as growth inhibition treated every 48 hrs measured after 96 hrs by CellTiter-Glo assay
Antiproliferative activity against human OCI-LY3 cells assessed as growth inhibition treated every 48 hrs measured after 96 hrs by CellTiter-Glo assay
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[PMID: 30954428] |
Z-VRPR-FMK (50 μM, 24 h) can effectively reduce the level of c-REL in the nucleus of HBL-1 cells and inhibit the signal transduction of NF-κB[2].
Z-VRPR-FMK (50 μM, 48 h) can inhibit the proliferation of ABC-DLBCL cell lines HBL-1, TMD8, OCI-Ly3 and OCI-Ly10[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1381885-28-4
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Appearance Solid
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Molecular Weight 676.78
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Formula C31H49FN10O6
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Color White to off-white
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Sequence
{Cbz}-Val-Arg-Pro-Arg-{FMK}
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Sequence Shortening
{Cbz}-VRPR-{FMK}
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (147.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jianglong Feng, et al. Z-VRPR-FMK can inhibit the growth and invasiveness of diffuse large B-cell lymphoma by depressing NF-κB activation and MMP expression induced by MALT1. Int J Clin Exp Pathol. 2019 Jun 1;12(6):1947-1955. [Content Brief]
[2]. Lorena Fontan, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4776 mL | 7.3879 mL | 14.7758 mL | 36.9396 mL |
| 5 mM | 0.2955 mL | 1.4776 mL | 2.9552 mL | 7.3879 mL | |
| 10 mM | 0.1478 mL | 0.7388 mL | 1.4776 mL | 3.6940 mL | |
| 15 mM | 0.0985 mL | 0.4925 mL | 0.9851 mL | 2.4626 mL | |
| 20 mM | 0.0739 mL | 0.3694 mL | 0.7388 mL | 1.8470 mL | |
| 25 mM | 0.0591 mL | 0.2955 mL | 0.5910 mL | 1.4776 mL | |
| 30 mM | 0.0493 mL | 0.2463 mL | 0.4925 mL | 1.2313 mL | |
| 40 mM | 0.0369 mL | 0.1847 mL | 0.3694 mL | 0.9235 mL | |
| 50 mM | 0.0296 mL | 0.1478 mL | 0.2955 mL | 0.7388 mL | |
| 60 mM | 0.0246 mL | 0.1231 mL | 0.2463 mL | 0.6157 mL | |
| 80 mM | 0.0185 mL | 0.0923 mL | 0.1847 mL | 0.4617 mL | |
| 100 mM | 0.0148 mL | 0.0739 mL | 0.1478 mL | 0.3694 mL |