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JAMM protein inhibitor 2

Cat No.:V46295 Purity: ≥98%
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor (antagonist) with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2 respectively.
JAMM protein inhibitor 2
JAMM protein inhibitor 2 Chemical Structure CAS No.: 848249-35-4
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
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Product Description
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor (antagonist) with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2 respectively. JAMM protein inhibitor 2 may be utilized in anti-cancer research.
JAMM protein inhibitor 2 (CAS 848249-35-4, compound 180) is a potent JAMM protease inhibitor. It has a molecular formula of C21H26N2O2 and a molecular weight of 338.44. The compound shows inhibitory activity against thrombin, Rpn11, and MMP2. It may be utilized in anti-cancer research.
Biological Activity I Assay Protocols (From Reference)
Targets
JAMM protein inhibitor 2 targets JAMM (JAB1/MPN/Mov34) proteases, which are involved in protein degradation, DNA repair, and cell cycle progression. It has IC50 values of 10 µM for thrombin, 46 µM for Rpn11, and 89 µM for MMP2. By inhibiting these targets, the compound may have therapeutic potential in cancer and other diseases related to dysregulated protein homeostasis.
ln Vitro
In vitro, JAMM protein inhibitor 2 is a potent inhibitor of JAMM proteases. It shows IC50 values of 10 µM for thrombin, 46 µM for Rpn11, and 89 µM for MMP2. These activities suggest its potential in anti-cancer research. However, detailed in vitro activity data against other targets are not extensively reported.
ln Vivo
In vivo, JAMM protein inhibitor 2 is expected to show efficacy in animal models of cancer by inhibiting JAMM protease activity. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature. The compound is primarily used as a research tool.
Enzyme Assay
In vitro enzyme assays for JAMM protein inhibitor 2 involve protease activity assays using purified recombinant enzymes such as thrombin, Rpn11, and MMP2. The compound is incubated with the enzyme and a specific fluorogenic or chromogenic substrate. The inhibition of substrate cleavage is measured, and IC50 values are determined from dose-response curves.
Cell Assay
In vitro cellular assays for JAMM protein inhibitor 2 are performed using cancer cell lines to assess its antiproliferative effects. Cells are treated with various concentrations of the compound. Cell viability and proliferation are assessed using standard assays like MTT or CellTiter-Glo. However, specific cellular assay protocols for this compound are not extensively reported.
Animal Protocol
In vivo animal studies with JAMM protein inhibitor 2 would typically be conducted in mouse xenograft models of cancer to evaluate its antitumor efficacy. The compound would be administered, and tumor growth inhibition would be assessed. However, specific protocols are not detailed in the available literature.
ADME/Pharmacokinetics
The pharmacokinetic properties of JAMM protein inhibitor 2 are not extensively reported. It has a molecular weight of 338.44. It is soluble in DMSO. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
Toxicity/Toxicokinetics
The toxicity profile of JAMM protein inhibitor 2 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
References

[1]. Methods and compositions for jamm protease inhibition. WO2013123071A1 (compound 180).

Additional Infomation
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 µM (thrombin), 46 µM (Rpn11), and 89 µM (MMP2). It has potential applications in anti-cancer research. The compound is available for research purposes only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H26N2O2
Molecular Weight
338.443345546722
Exact Mass
338.199
CAS #
848249-35-4
PubChem CID
4853066
Appearance
Light yellow to brown solid powder
LogP
4.6
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
6
Heavy Atom Count
25
Complexity
422
Defined Atom Stereocenter Count
0
SMILES
O=C(COC1C(CC)=CC=CC=1)NC1C(C)=CC(N2CCCC2)=CC=1
InChi Key
BWVQJXWDZCDJJJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H26N2O2/c1-3-17-8-4-5-9-20(17)25-15-21(24)22-19-11-10-18(14-16(19)2)23-12-6-7-13-23/h4-5,8-11,14H,3,6-7,12-13,15H2,1-2H3,(H,22,24)
Chemical Name
2-(2-ethylphenoxy)-N-(2-methyl-4-pyrrolidin-1-ylphenyl)acetamide
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

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)
Solubility Data
Solubility (In Vitro)
DMSO : ~14.71 mg/mL (~43.46 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 1.47 mg/mL (4.34 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.7 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: 1.47 mg/mL (4.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.7 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.

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Solubility in Formulation 3: ≥ 1.47 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 14.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9547 mL 14.7737 mL 29.5473 mL
5 mM 0.5909 mL 2.9547 mL 5.9095 mL
10 mM 0.2955 mL 1.4774 mL 2.9547 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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