| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Cysteine cathepsin family (broad-spectrum). JPM-OEt binds covalently at the active site and irreversibly inhibits the cysteine cathepsin family. The compound has antitumor activity through inhibition of cathepsin-mediated tumor progression.
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|---|---|
| ln Vitro |
JPM-OEt is a broad-spectrum cysteine cathepsin inhibitor. It binds covalently at the active site and irreversibly inhibits the cysteine cathepsin family. The compound decreases tumor cathepsin B activity. Detailed in vitro potency against individual cathepsins has been reported.
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| ln Vivo |
JPM-OEt (50 mg/kg; intraperitoneal injection; once daily for 30 days) effectively lowers tumor cathepsin B activity [1]. JPM-OEt (50 mg/kg; i.p.; twice daily for 4 weeks) causes tumor regression in the RIP1-Tag2 (RT2) animal model of islet cell carcinogenesis [2]. JPM-OEt (50 mg/kg; i.p.; daily for 63 to 98 days) produces a considerable delay in the growth in tumor burden within the first 2 weeks of treatment [3].
JPM-OEt (50 mg/kg; i.p.; daily for 30 days) significantly decreases tumor cathepsin B activity. JPM-OEt (50 mg/kg; twice daily for 4 weeks) induces tumor regression in the RIP1-Tag2 (RT2) mouse model of pancreatic islet cell tumorigenesis. The compound exhibits strong antitumor effects in vivo. |
| Enzyme Assay |
Cathepsin enzymatic activity assay: Recombinant cysteine cathepsins are incubated with varying concentrations of JPM-OEt and a fluorogenic peptide substrate (e.g., Z-Phe-Arg-AMC for cathepsin B) in assay buffer at 37°C for 30–60 min. The release of fluorescent AMC is measured. IC50 values are calculated.
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| Cell Assay |
Tumor cathepsin B activity assay: Tumor-bearing mice are treated with JPM-OEt at 50 mg/kg i.p. daily for 30 days. Tumors are harvested, and cathepsin B activity in tumor lysates is measured using a fluorogenic substrate. The reduction in cathepsin B activity is calculated compared to vehicle-treated controls.
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| Animal Protocol |
Animal/Disease Models: Transgenic mice Female mice [3]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day from 63 to 98 days Experimental Results: The increase in tumor burden was Dramatically delayed during the first 2 weeks of treatment. However, no significant differences were detected between the two groups on days 84, 91, and 98. RIP1-Tag2 (RT2) mouse model of pancreatic islet cell tumorigenesis: RT2 transgenic mice that develop pancreatic islet cell tumors are treated with JPM-OEt at 50 mg/kg i.p. twice daily for 4 weeks. Tumor burden is assessed by histological analysis. Tumor regression is quantified and compared to vehicle-treated controls. |
| ADME/Pharmacokinetics |
JPM-OEt has a CAS number of 262381-84-0. The compound is a broad-spectrum cysteine cathepsin inhibitor with antitumor activity. Comprehensive PK parameters such as bioavailability and half-life have been characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published. JPM-OEt is for research use only. Standard laboratory safety practices should be followed when handling this compound. As a cysteine cathepsin inhibitor, potential effects on normal tissue remodeling should be considered.
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| References |
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| Additional Infomation |
JPM-OEt is a broad-spectrum, irreversible cysteine cathepsin inhibitor with antitumor activity. It decreases tumor cathepsin B activity (50 mg/kg i.p. daily for 30 days) and induces tumor regression in the RT2 mouse model of pancreatic cancer (50 mg/kg i.p. twice daily for 4 weeks). No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C20H28N2O6
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|---|---|
| Molecular Weight |
392.4461
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| Exact Mass |
392.195
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| CAS # |
262381-84-0
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| PubChem CID |
11257859
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| Appearance |
White to off-white solid powder
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| LogP |
1.694
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
545
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCOC(=O)[C@@H]1[C@H](O1)C(=O)N[C@@H](CC(C)C)C(=O)NCCC2=CC=C(C=C2)O
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| InChi Key |
VRFYYTLIPKHELT-ULQDDVLXSA-N
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| InChi Code |
InChI=1S/C20H28N2O6/c1-4-27-20(26)17-16(28-17)19(25)22-15(11-12(2)3)18(24)21-10-9-13-5-7-14(23)8-6-13/h5-8,12,15-17,23H,4,9-11H2,1-3H3,(H,21,24)(H,22,25)/t15-,16-,17-/m0/s1
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| Chemical Name |
ethyl (2S,3S)-3-(((S)-1-((4-hydroxyphenethyl)amino)-4-methyl-1-oxopentan-2-yl)carbamoyl)oxirane-2-carboxylate
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| Synonyms |
JPM-OEt JPM OEt JPMOEt JPM-565 Ethyl ester
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~318.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5481 mL | 12.7405 mL | 25.4810 mL | |
| 5 mM | 0.5096 mL | 2.5481 mL | 5.0962 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5481 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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