GSK2983559 free acid
Based on 2 publication(s) in Google Scholar
GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 1579965-12-0
- Formula: C21H23N4O7PS2
- Molecular Weight:538.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK2983559 free acid
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Biological Activity
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RIPK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
1.34 nM
Compound: 5; GSK2983559
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Antiinflammatory activity in MDP-stimulated IL-8 production in human THP-1 cells pretreated for 2 hrs followed by MDP stimulation for 6 hrs
Antiinflammatory activity in MDP-stimulated IL-8 production in human THP-1 cells pretreated for 2 hrs followed by MDP stimulation for 6 hrs
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[PMID: 36058467] |
GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:1-1024 nM
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Incubation Time:2 hours
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Result:Inhibited IL-8 production with an IC50 of 1.34 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (female) injected with MDP (100 μg)[2]
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Dosage:3 and 10 mg/kg
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Administration:Oral gavage; 3 and 10 mg/kg; once
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Result:Suppressed serum IL-6 levels in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1579965-12-0
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Appearance Solid
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Molecular Weight 538.53
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Formula C21H23N4O7PS2
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Color Light yellow to yellow
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SMILES
CC(C)(C)S(C(C(OCCOP(O)(O)=O)=CC1=NC=N2)=CC1=C2NC3=CC(N=CS4)=C4C=C3)(=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
Solvent & Solubility
DMSO : 5 mg/mL (9.28 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Haile PA, et al. Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases. J Med Chem. 2019 Jul 25;62(14):6482-6494. [Content Brief]
[2]. Shuwei Wu, et al. Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors. Bioorg Med Chem Lett. 2022 Sep 2;75:128968. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8569 mL | 9.2845 mL | 18.5691 mL | 46.4227 mL |
| 5 mM | 0.3714 mL | 1.8569 mL | 3.7138 mL | 9.2845 mL |
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