GSK583
Based on 9 publication(s) in Google Scholar
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 1346547-00-9
- Formel: C20H19FN4O2S
- Molecular Weight:398.45
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) GSK583
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Death Dis. 2026 May 29. [Abstract]
- Chin Med. 2026 Apr 17;21(1):119. [Abstract]
- Biomater Sci. 2019 Jul 1;7(7):2702-2715. [Abstract]
- J Biol Chem. 2023 Nov;299(11):105253. [Abstract]
- J Immunol. 2017 May 1;198(9):3729-3736. [Abstract]
- Infect Immun. 2021 Jul 15;89(8):e0014121. [Abstract]
- PLoS One. 2026 Jan 21;21(1):e0341445. [Abstract]
- Research Square Preprint. 2020 Dec.
Customer Validation & Images
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IF
Biologische Aktivität
IC50: 5 nM (RIP2K)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10000 nM
Compound: 27
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Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion
Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion
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[PMID: 27109867] |
| HEK293 | IC50 |
18 nM
Compound: 27
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Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion
Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion
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[PMID: 27109867] |
| Monocyte | IC50 |
8 nM
Compound: 27
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Inhibition of MDP-stimulated TNF-alpha release in human monocytes preincubated for 30 mins prior to MDP stimulation measured after 6 hrs by immunoassay
Inhibition of MDP-stimulated TNF-alpha release in human monocytes preincubated for 30 mins prior to MDP stimulation measured after 6 hrs by immunoassay
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[PMID: 27109867] |
GSK583 (1 μM) exhibits excellent selectivity in a panel of 300 kinases, including p38α and VEGFR2. GSK583 potently and dose dependently inhibits MDP-stimulated tumor necrosis factor-alpha (TNFα) production with an IC50 of 8 nM. GSK583 demonstrates only a modest reduction in potency when profiled in a similar MDP-induced TNFα production assay in human whole blood (IC50 = 237 nM) and rat whole blood (IC50 = 133 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1346547-00-9
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Appearance Solid
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Molecular Weight 398.45
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Formel C20H19FN4O2S
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Color Light yellow to yellow
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SMILES
FC1=CC2=C(NN=C2NC3=CC=NC4=CC=C(S(=O)(C(C)(C)C)=O)C=C34)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Dis
Ripk2 promotes CD8+ T cell inactivation and hepatocellular carcinoma progression through Myb/Cxcl9 and Pax5/Adpgk signaling pathways. [Abstract]2026 May 29. PMID: 42215445 -
Chin Med
Thlaspi arvense attenuates colitis-associated colorectal tumorigenesis through suppression of neutrophil recruitment via the NOD/NF-κB pathway. [Abstract]2026 Apr 17;21(1):119. PMID: 41998751 -
Biomater Sci
2019 Jul 1;7(7):2702-2715. PMID: 31065630 -
J Biol Chem
The kinesin-14 family motor protein KIFC2 promotes prostate cancer progression by regulating p65. [Abstract]2023 Nov;299(11):105253. PMID: 37716704 -
J Immunol
2017 May 1;198(9):3729-3736. PMID: 28330897
GSK583 purchased from MedChemExpress. Usage Cited in: J Immunol. 2017 May 1;198(9):3729-3736. [Abstract]
Confocal images of lysozyme and procryptdin in cultured WT crypt organoids treated with GSK583 (5 μM) or mock-treated (A), or WEHI-345 (2.5 μM) or mock-treated (B) for 16 hours.
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Infect Immun
Bartonella henselae Persistence within Mesenchymal Stromal Cells Enhances Endothelial Cell Activation and Infectibility That Amplifies the Angiogenic Process. [Abstract]2021 Jul 15;89(8):e0014121. PMID: 34031126 -
PLoS One
RIPK2 induces docetaxel resistance in prostate cancer through the NF-κB/P-gp signaling pathway. [Abstract]2026 Jan 21;21(1):e0341445. PMID: 41563982 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (250.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
A fluorescent polarization based binding assay is developed to quantitate interaction of novel test compounds at the ATP binding pocket of RIP2K by competition with a fluorescently labeled ATP competitive ligand. Full length FLAG His tagged RIP2K is purified from a baculovirus expression system and is used at a final assay concentration of twice the KD apparent. A fluorescent labeled ligand that is reversible and competitive with the inhibitors is used at a final assay concentration of 5 nM. Both the enzyme and ligand are prepared in solutions in 50 mM HEPES pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, and 1 mM CHAPS. Test compounds are prepared in 100% DMSO, and 100 nL is dispensed to individual wells of a multiwell plate. Next, 5 μL of RIP2K is added to the test compounds at twice the final assay concentration and incubated at room temperature for 10 min. Following the incubation, 5 μL of the fluorescent labeled ligand solution is added to each reaction at twice the final assay concentration and incubated at room temperature for at least 10 min. Finally, samples are read on an instrument capable of measuring fluorescent polarization. Test compound inhibition is expressed as percent (%) inhibition of internal assay controls. For concentration response experiments, normalized data are fit using the following four parameter logistic equation: y = A + ((B-C))/(1+(10x)/(10C)D), where y is the % activity (% inhibition) at a specified compound concentration, A is the minimum % activity, B is the maximum % activity, C = log10(IC50), D = Hill slope, x = log10(compound concentration [M]), and pIC50 = (−C).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female C57Bl/6 mice (for cytokine analyses) or male Balb/c mice (for peritoneal neutrophil analyses) (n=10/treatment group) are dosed orally 15 min prior to MDP challenge with vehicle or GSK583 (0.1, 1, or 10 mg/kg). For peritoneal neutrophil analysis, mice are sacrificed at 4 h post-MDP challenge (30 μg, i.p.) and peritoneal fluid is collected by lavage. Peritoneal neutrophils are quantified by FACS analysis.
Rats[1]
Female Crl:CD(SD) rats (n=8/treatment group) are dosed orally with vehicle or GSK583 15 min prior to MDP challenge (150 μg/rat, IV). At 2 h post MDP challenge, rats are sacrificed and terminal serum is prepared from blood collected via cardiac stick. Serum cytokine levels (IL-6, IL-8 or KC, IL-1β, and TNFα) are quantified by the MSD platform.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (283 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)
Verweise
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5097 mL | 12.5486 mL | 25.0973 mL | 62.7431 mL |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0195 mL | 12.5486 mL | |
| 10 mM | 0.2510 mL | 1.2549 mL | 2.5097 mL | 6.2743 mL | |
| 15 mM | 0.1673 mL | 0.8366 mL | 1.6732 mL | 4.1829 mL | |
| 20 mM | 0.1255 mL | 0.6274 mL | 1.2549 mL | 3.1372 mL | |
| 25 mM | 0.1004 mL | 0.5019 mL | 1.0039 mL | 2.5097 mL | |
| 30 mM | 0.0837 mL | 0.4183 mL | 0.8366 mL | 2.0914 mL | |
| 40 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5686 mL | |
| 50 mM | 0.0502 mL | 0.2510 mL | 0.5019 mL | 1.2549 mL | |
| 60 mM | 0.0418 mL | 0.2091 mL | 0.4183 mL | 1.0457 mL | |
| 80 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6274 mL |
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