Free shipping on all orders over $ 500


Cat. No. M5232
GSK583 Structure
Size Price Availability Quantity
2mg USD 85 In stock
5mg USD 157 In stock
10mg USD 247 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: GSK583 possesses comparable binding affinity for RIP3 kinase as demonstrated by an in-house FP binding assay configured similarly to the RIP2 FP assay (RIP2 FP IC50 = 5 nM; RIP3 FP IC50 = 16 nM). Despite this potent biochemical activity against RIP3 kinase, GSK583 shows little or no inhibition of RIP3-dependent necroptotic cell death in a cellular assay up to 10 μM concentration. GSK583 potently and dose dependently inhibits MDP-stimulated tumor necrosis factor-alpha (TNFα) production with an IC50 = 8 nM in primary human monocytes. Following treatment with GSK583 at 1 μM, little inhibition of pro-inflammatory signaling is observed upon activation of Toll-like receptors (TLR2, TLR4, TLR7) or cytokine receptors (IL-1R, TNFR) but complete inhibition is observed upon activation of both NOD1 and NOD2 receptors, which signal in a RIP2-dependent manner. Although GSK583 has excellent kinase selectivity, it does inhibit both the hERG channel and Cyp3A4, which precludes it from further progression as a drug candidate. In vivo: GSK583 has low clearance, moderate volumes of distribution, and moderate oral bioavailability in both rat and mouse. Eventhough GSK583 would not produce a human phamacodynamic response within an acceptable dose range which precludes this molecule from further development as a drug candidate, the oral PK in rat and mouse provides sufficient systemic exposure for use as a preclinical in vivo tool molecule in an acute inflammation challenge mode.

Cell Experiment
Cell lines primary human monocytes
Preparation method To assess cellular selectivity, monocytes are pretreated with inhibitor for 30 min, then stimulated for 6 h with ligands which selectively agonize NLRs NOD1, NOD2; Toll-like receptors TLR, TLR4, TLR7, or cytokine receptors IL-1R, TNFR. Release of pro-inflammatory cytokines, either TNFα (NOD2, TLR2, TLR4, IL1R) or IL-8 (NOD1, TLR7, TNFR), is measured by immunoassay. Percent inhibition and/or IC50 values are calculated.
Concentrations 1 μM
Incubation time 30 min
Animal Experiment
Animal models C57BL/6 mice
Dosages 0.1, 1, 10 and 100 mg/kg
Administration oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 398.45
Formula C20H19FN4O2S
CAS Number 1346547-00-9
Purity >98%
Solubility 79 mg/mL in DMSO
Storage at -20°C

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Haile PA, et al. J Med Chem. 2016 May 26;59(10):4867-80. PMID: 27109867.

Related NF-κB Products

AZD3264 is a novel IKK2 inhibitor.


Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.

Dimethyl Fumarate

Dimethyl fumarate(DMF) is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator; induces upregulation of antioxidant gene expression.

5-Aminosalicylic acid

5-Aminosalicylic acid is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.


SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM.

Abmole Inhibitor Catalog 2017

Keywords: GSK583 supplier, NF-κB, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.