| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| 5mg | |||
| Other Sizes |
| Targets |
Cathepsin B cathepsin L
Cathepsin B (Cat-B), Cathepsin L (Cat-L) |
|---|---|
| ln Vitro |
The cleavage of the probe Ac-PLVQ-AMC by human recombinant CtsB and L is significantly influenced by Ac-VLPE-FMK (2 μM) [1]. In 769-p and A498 cells, Ac-VLPE-FMK (30 min) inhibits fluorescence that is generated by cleavage of the substrate Ac-PLVQ-AMC [1]. Ac-VLPE-FMK (2.5-250 μM; 24-72 h) influences the migration rate, adhesion, colony formation, and marker expression of renal cancer cells, but not their viability [1].
Ac-VLPE-FMK is an inhibitor of Cathepsin B and Cathepsin L. At 2 microM, it significantly affects the cleavage of the probe Ac-PLVQ-AMC by recombinant human CtsB and L. It inhibits fluorescence from substrate cleavage in 769-p and A498 renal cancer cells after 30 minutes. At 2.5-250 microM (24-72 h), it alters cell migration rate, adhesion, colony formation, and marker expression. |
| ln Vivo |
Currently, no specific in vivo data is available for this compound. General in vivo information for similar cathepsin inhibitors may include their ability to reduce tumor growth and metastasis in mouse xenograft models, or to protect against ischemia-reperfusion injury.
|
| Enzyme Assay |
A typical enzyme inhibition assay for cathepsins B and L uses fluorogenic substrates like Z-Arg-Arg-AMC (for Cat-B) and Z-Phe-Arg-AMC (for Cat-L). The compound is pre-incubated with the enzyme in an activation buffer (e.g., 100 mM sodium acetate, pH 5.5, 5 mM DTT) at 37degC. Substrate is added, and fluorescence is monitored (Ex/Em=380/460 nm).
|
| Cell Assay |
General cellular protocols use renal cancer cell lines (e.g., 769-p, A498). Cells are treated with Ac-VLPE-FMK (2.5-250 microM) for 24-72 hours. Cell viability is measured by MTT assay, but the compound primarily affects cell functions like migration, adhesion, and colony formation rather than viability. Western blotting is used to assess marker expression.
|
| Animal Protocol |
General in vivo procedures for cathepsin inhibitors involve using a mouse xenograft model. Tumor-bearing mice are treated with the compound via intraperitoneal injection daily for 2-4 weeks. Tumor volume is measured with calipers, and tumors are harvested post-mortem for IHC analysis of proliferation (Ki-67) and apoptosis (cleaved caspase-3).
|
| ADME/Pharmacokinetics |
Ac-VLPE-FMK has a molecular weight of 528.61. As a tetrapeptide, it is likely to be rapidly cleared and have a short half-life in vivo. The FMK group is designed for irreversible covalent inhibition, leading to sustained target engagement. For in vivo use, it is typically formulated in DMSO, PEG300, and saline.
|
| Toxicity/Toxicokinetics |
As a research compound, specific toxicity data for Ac-VLPE-FMK is not publicly available. The FMK group is known to be reactive and can potentially label off-target proteins if used at high concentrations, which is a common consideration for covalent inhibitors. Standard lab safety precautions apply.
|
| References | |
| Additional Infomation |
Ac-VLPE-FMK is a research tool used to study the role of cathepsins B and L in cancer biology. It is used to investigate cancer aggressiveness, particularly in renal cell carcinoma. It has not progressed to clinical trials or been approved for therapeutic use.
|
| Molecular Formula |
C25H41FN4O7
|
|---|---|
| Molecular Weight |
528.614050626755
|
| Exact Mass |
528.295
|
| CAS # |
2679825-27-3
|
| PubChem CID |
168355663
|
| Appearance |
White to off-white solid powder
|
| LogP |
0
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
37
|
| Complexity |
849
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC(C)C[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)OC)C(=O)CF)NC(=O)[C@H](C(C)C)NC(=O)C
|
| InChi Key |
MDAFONIYDVLMOY-OZIGNCPNSA-N
|
| InChi Code |
InChI=1S/C25H41FN4O7/c1-14(2)12-18(29-24(35)22(15(3)4)27-16(5)31)25(36)30-11-7-8-19(30)23(34)28-17(20(32)13-26)9-10-21(33)37-6/h14-15,17-19,22H,7-13H2,1-6H3,(H,27,31)(H,28,34)(H,29,35)/t17-,18-,19-,22-/m0/s1
|
| Chemical Name |
methyl (4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-6-fluoro-5-oxohexanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8918 mL | 9.4588 mL | 18.9175 mL | |
| 5 mM | 0.3784 mL | 1.8918 mL | 3.7835 mL | |
| 10 mM | 0.1892 mL | 0.9459 mL | 1.8918 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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