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RIP2 kinase inhibitor 1

Catalog No.GC32775

RIP2 kinase inhibitor 1 is an active metabolite of GSK2983559. RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

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RIP2 kinase inhibitor 1 Chemical Structure

Cas No.: 1423186-80-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$109.00
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1mg
$43.00
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5mg
$108.00
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10mg
$171.00
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50mg
$585.00
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100mg
$945.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

Rats[1] Rats are orally pre-dosed with RIP2 kinase inhibitor 1, at a dose of 2 mg/kg (8 rats) and with Prednisolone (8 rats, used as a positive control), followed by dosing with L18-MDP (50 μg/rat) 0.25 h/min after pre-dosing. Combined cytokine levels (IL8, TNFa, IL6 and IL-Ιβ) in whole blood samples taken from the rats in this study are measured using an antibody based detection. The combined cytokine response is calculated as the averaged response for the 4 cytokines measured relative to the response observed in the vehicle-treated mice, and are depicted as the mean±standard error of the mean (n=8 rats/group).

References:

[1]. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.

Background

RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

RIP2 kinase inhibitor 1 is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase, which is also referred to as CARD3, RICK, CARDIAK, or RIPK2, is a TKL family serine/threonine protein kinase involved in innate immune signaling. RIP2 kinase is composed of an N-terminal kinase domain and a C-terminal caspase-recruitment domain (CARD) linked via an intermediate (IM) region. The CARD domain of RIP2 kinase mediates interaction with other CARD-containing proteins, such as NODI and NOD2. NODI and NOD2 are cytoplasmic receptors which play a key role in innate immune surveillance. They recognize both gram positive and gram negative bacterial pathogens and are activated by specific peptidoglycan motifs, diaminopimelic acid (i.e., DAP) and muramyl dipeptide[1].

[1]. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.

Chemical Properties

Cas No. 1423186-80-4 SDF
Canonical SMILES CC(C)(C)S(C1=C(OCCO)C=C(N=CN=C2NC3=CC(N=CS4)=C4C=C3)C2=C1)(=O)=O
Formula C21H22N4O4S2 M.Wt 458.55
Solubility DMSO : ≥ 32 mg/mL (69.79 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1808 mL 10.9039 mL 21.8079 mL
5 mM 0.4362 mL 2.1808 mL 4.3616 mL
10 mM 0.2181 mL 1.0904 mL 2.1808 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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