| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
RIPK2-IN-3 targets receptor-interacting serine/threonine protein kinase 2 (RIPK2). RIPK2 is a key mediator of inflammatory signaling pathways, particularly in the NOD1/NOD2 signaling cascade. By inhibiting RIPK2, the compound blocks the activation of NF-κB and other inflammatory pathways, leading to anti-inflammatory and anti-tumor effects. The compound inhibits recombinant truncated RIPK2 with an IC50 of 6.39 μM.
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|---|---|
| ln Vitro |
In cell-free biochemical assays, RIPK2-IN-3 inhibits recombinant truncated RIPK2 with an IC50 of 6.39 μM. This activity demonstrates the compound's direct inhibition of RIPK2 enzymatic activity. The compound also potently inhibits the proliferation of cancer cells by >70% and inhibits NF-κB activity. These activities contribute to its potential as an anti-inflammatory and anti-tumor agent.
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| ln Vivo |
In cell-based assays, RIPK2-IN-3 potently inhibits the proliferation of cancer cells by >70% and inhibits NF-κB activity. The compound's anti-inflammatory and anti-tumor activities are mediated through RIPK2 inhibition. The compound can be used for research of inflammation and cancer. Its effects on cell proliferation and NF-κB signaling are evaluated in various cell lines.
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| Enzyme Assay |
The cell-free assay for RIPK2 inhibition typically involves measuring the kinase activity of purified recombinant truncated RIPK2 in the presence of the compound. The assay uses a peptide substrate and ATP, and the phosphorylation of the substrate is measured using radioactivity, fluorescence, or luminescence. The IC50 of 6.39 μM is determined from dose-response curves. The compound's selectivity can be assessed by testing against a panel of other kinases.
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| Cell Assay |
Cell-based assays for RIPK2-IN-3 involve culturing cancer cell lines and treating them with the compound at concentrations ranging from 0.1 to 100 μM. Cells are incubated for 24-72 hours, and cell proliferation is assessed using MTT or CCK-8 assays. NF-κB activity is measured using reporter assays or by assessing the expression of NF-κB target genes by qRT-PCR. The compound's effects on inflammatory cytokine production can also be measured.
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| Animal Protocol |
In animal models, RIPK2-IN-3 has been evaluated for its anti-inflammatory and anti-tumor activity. Typical studies involve administration of the compound to mice via intraperitoneal or oral routes. Inflammatory disease models are used to assess the compound's ability to reduce inflammation. Tumor-bearing mice are used to assess anti-tumor efficacy. Tissues are collected for analysis of RIPK2 inhibition, NF-κB activity, and inflammatory markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RIPK2-IN-3 have not been extensively reported. As a small molecule with a molecular weight of 410.47 g/mol, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound has a predicted LogP of 3.46 and is soluble in DMSO. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
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| Toxicity/Toxicokinetics |
RIPK2-IN-3 is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a RIPK2 inhibitor, the compound may have effects on immune and inflammatory pathways. Standard toxicity studies in rodents would be required to determine the maximum tolerated dose, target organ toxicity, and safety profile.
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| References | |
| Additional Infomation |
RIPK2-IN-3 is a research-grade compound supplied for inflammation and cancer research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a potent RIPK2 inhibitor with an IC50 of 6.39 μM. It potently inhibits the proliferation of cancer cells by >70% and inhibits NF-κB activity. This product is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C25H22N4O2
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|---|---|
| Molecular Weight |
410.47
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| Exact Mass |
410.174
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| CAS # |
1290490-78-6
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| PubChem CID |
99506096
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.641
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| LogP |
3.46
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
621
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(C)=C(C=1)NC(C1C=CC=CC=1)=O)NC1=CC=CC(=C1)C1=NC=CN1C
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| InChi Key |
OIIYBZHRYXJCHR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H22N4O2/c1-17-11-12-20(16-22(17)28-24(30)18-7-4-3-5-8-18)25(31)27-21-10-6-9-19(15-21)23-26-13-14-29(23)2/h3-16H,1-2H3,(H,27,31)(H,28,30)
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| Chemical Name |
3-benzamido-4-methyl-N-[3-(1-methylimidazol-2-yl)phenyl]benzamide
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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 |
| 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) |
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
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| 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 | 2.4362 mL | 12.1812 mL | 24.3623 mL | |
| 5 mM | 0.4872 mL | 2.4362 mL | 4.8725 mL | |
| 10 mM | 0.2436 mL | 1.2181 mL | 2.4362 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.
Products are for research use only; We do not sell to patients
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