| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
RIPK2-IN-2 targets receptor-interacting protein 2 (RIP2) kinase, a serine/threonine protein kinase that plays a critical role in innate immune signaling. RIP2 is activated upon binding to NOD1 or NOD2, which are intracellular receptors that recognize bacterial peptidoglycan fragments. Once activated, RIP2 acts as a molecular scaffold to connect other kinases (TAK1, IKKα/β/γ) involved in mitogen-activated protein kinase (MAPK) activation and NF-κB signaling. By inhibiting RIP2 kinase, RIPK2-IN-2 blocks this signaling pathway, thereby reducing the production of pro-inflammatory cytokines.
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| ln Vitro |
RIP2 kinase inhibitor 2 is a brand-new quinazolylamine prodrug that stops RIP2 kinase from working. A serine/threonine protein kinase belonging to the TKL family, receptor-interacting protein 2 (RIP2) kinase is implicated in innate immunological signaling. When RIP2 kinase is activated, it binds to either NODI or NOD2, and its main role is to act as a molecular scaffold to connect other kinases (TAK1, IKKα/β/γ) that are involved in mitogen-activated protein kinase activation and NF-κB [1].
In vitro, RIPK2-IN-2 is a potent inhibitor of RIP2 kinase activity. It is a quinazolylamine prodrug that inhibits RIP2 kinase. Its ability to inhibit RIP2 kinase has been confirmed in biochemical assays. However, specific IC50 values are not detailed in standard product descriptions. The compound is used in cell-based assays to study the effects of RIP2 kinase inhibition on immune cell signaling. By inhibiting RIP2, it is expected to reduce the production of pro-inflammatory cytokines in response to NOD1/2 activation. |
| ln Vivo |
In vivo, RIPK2-IN-2 is a research compound used to study the role of RIP2 kinase in inflammation. By inhibiting RIP2, it can modulate immune responses and reduce inflammation in animal models of inflammatory diseases. However, specific in vivo protocols and results, such as efficacy in disease models, are not detailed in the available literature. Its use is limited to research applications to validate RIP2 kinase as a therapeutic target.
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| Enzyme Assay |
The in vitro assays for RIPK2-IN-2 measure its inhibition of RIP2 kinase activity. Kinase assays are performed using recombinant RIP2 kinase, a peptide substrate, and ATP in the presence of varying concentrations of RIPK2-IN-2. The incorporation of phosphate into the substrate is measured, and the IC50 is determined from the dose-response curve. These assays confirm the compound's potency at its molecular target. Selectivity can be assessed by testing the compound against a panel of other kinases.
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| Cell Assay |
In vitro cell-based assays for RIPK2-IN-2 are used to study its effects on NOD1/2-mediated signaling and inflammation. In a typical assay, immune cells, such as macrophages, are stimulated with a NOD2 agonist (e.g., muramyl dipeptide, MDP) in the presence or absence of RIPK2-IN-2. The production of pro-inflammatory cytokines, such as TNF-α and IL-6, is measured by ELISA. The phosphorylation of downstream signaling molecules, such as NF-κB and MAPK, can also be assessed by Western blotting. These assays confirm that RIPK2-IN-2 inhibits RIP2-mediated inflammatory responses.
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| Animal Protocol |
In vivo animal experiments for RIPK2-IN-2 are conducted in models of inflammatory diseases, such as colitis or arthritis, where NOD1/2 signaling plays a role. In a typical study, RIPK2-IN-2 is administered orally or by injection to animals with induced inflammation. Inflammatory parameters, such as cytokine levels, tissue damage, and clinical scores, are assessed. However, specific protocols for RIPK2-IN-2 are not detailed in the available literature. Its use is limited to research applications.
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| ADME/Pharmacokinetics |
RIPK2-IN-2 has a molecular weight of 432.54 g/mol and a molecular formula of C21H28N4O4S. It has a logP of 3.27. It is a light yellow to yellow solid powder. It is soluble in DMSO (5 mg/mL). For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for RIPK2-IN-2 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. The compound is a selective inhibitor of RIP2 kinase, and its toxicity would be related to its effects on RIP2-mediated signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling RIPK2-IN-2. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
RIPK2-IN-2 is a research compound and is not approved for any clinical or therapeutic use. It is a potent and selective inhibitor of receptor-interacting protein 2 (RIP2) kinase. RIP2 is a serine/threonine protein kinase involved in innate immunological signaling, acting as a molecular scaffold downstream of NOD1/2 receptors. By inhibiting RIP2, RIPK2-IN-2 blocks the activation of NF-κB and MAPK pathways, reducing the production of pro-inflammatory cytokines. It is used as a research tool to study the role of RIP2 kinase in immune cell signaling and inflammation and to validate RIP2 as a therapeutic target for inflammatory diseases.
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| Molecular Formula |
C21H28N4O4S
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| Molecular Weight |
432.5364
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| Exact Mass |
432.183
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| CAS # |
1581270-11-2
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| PubChem CID |
73426595
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
670.0±55.0 °C at 760 mmHg
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| Flash Point |
359.0±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
3.27
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
663
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(NN=C1NC2=C3C=C(C(=CC3=NC=C2)OCCOC)S(=O)(=O)C(C)(C)C)C
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| InChi Key |
QODPGRHWJBWTJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H28N4O4S/c1-13-14(2)24-25-20(13)23-16-7-8-22-17-12-18(29-10-9-28-6)19(11-15(16)17)30(26,27)21(3,4)5/h7-8,11-12H,9-10H2,1-6H3,(H2,22,23,24,25)
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| Chemical Name |
6-tert-butylsulfonyl-N-(4,5-dimethyl-1H-pyrazol-3-yl)-7-(2-methoxyethoxy)quinolin-4-amine
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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) |
DMSO : ~5 mg/mL (~11.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.16 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 5.0 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: ≥ 0.5 mg/mL (1.16 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 5.0 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: ≥ 0.5 mg/mL (1.16 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 | 2.3119 mL | 11.5596 mL | 23.1192 mL | |
| 5 mM | 0.4624 mL | 2.3119 mL | 4.6238 mL | |
| 10 mM | 0.2312 mL | 1.1560 mL | 2.3119 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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