GSK583, with the chemical formula C21H23FN4O and a molecular weight of 370.44 g/mol, is a highly selective and potent inhibitor of RIP2 kinase, a central component of the innate immune system. It effectively blocks NOD2 signaling by interfering with XIAP-RIP2 binding, leading to decreased cytokine and chemokine production. GSK583 exhibits an IC50 of 5 nM for human RIP2 kinase and 2 nM for rat RIP2 kinase, while also potently inhibiting isolated RIP3 kinase (IC50 = 5 nM) but remains inactive against RIP3 in cellular assays due to a very low KM,ATP.
1346547-00-9
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Basic information
- Product Name: GSK583
- Synonyms: GSK583;SK583
- CAS NO:1346547-00-9
- Molecular Formula: C20H19FN4O2S
- Molecular Weight: 398.4538632
- EINECS: -0
- Product Categories: N/A
- Mol File: 1346547-00-9.mol
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Chemical Properties
- Melting Point: N/A
- Boiling Point: 652.9±55.0 °C(Predicted)
- Flash Point: N/A
- Appearance: /
- Density: 1.402±0.06 g/cm3(Predicted)
- Refractive Index: N/A
- Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
- Solubility: Soluble in DMSO (up to at least 25 mg/ml).
- PKA: 12.59±0.40(Predicted)
- Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
- CAS DataBase Reference: GSK583(CAS DataBase Reference)
- NIST Chemistry Reference: GSK583(1346547-00-9)
- EPA Substance Registry System: GSK583(1346547-00-9)
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Safety Data
- Hazard Codes: N/A
- Statements: N/A
- Safety Statements: N/A
- WGK Germany:
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 1346547-00-9(Hazardous Substances Data)
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1346547-00-9 Usage
Uses
Used in Pharmaceutical Industry:GSK583 is used as a research compound for studying the role of RIP2 kinase in inflammatory and immune responses. Its ability to selectively inhibit RIP2 kinase makes it a valuable tool in understanding the underlying mechanisms of various inflammatory diseases and immune system disorders.
Used in Inflammatory Disease Research:
GSK583 is used as a therapeutic agent for the treatment of inflammatory diseases, as its inhibition of RIP2 kinase can potentially reduce the production of inflammatory cytokines and chemokines, thereby alleviating disease symptoms and progression.
Used in Immune System Disorders Research:
GSK583 is used as a research tool to investigate the role of RIP2 kinase in immune system disorders, such as autoimmune diseases and immune deficiencies. Its selective inhibition of RIP2 kinase can provide insights into the development of novel therapeutic strategies for these conditions.
Used in Drug Development:
GSK583 is used as a lead compound in the development of new drugs targeting RIP2 kinase for the treatment of inflammatory diseases and immune system disorders. Its high selectivity and potency make it a promising candidate for further optimization and development into a clinically relevant drug.
References
1) Haile?et al.?(2016),?The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinoline-4-amine; J. Med. Chem.,?59?4867 2) Goncharov?et al.?(2018),?Disruption of XIAP-RIP2 Association Blocks NOD2-Mediated Inflammatory Signaling; Mol. Cell,?69?551Check Digit Verification of cas no
The CAS Registry Mumber 1346547-00-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,4,6,5,4 and 7 respectively; the second part has 2 digits, 0 and 0 respectively.Calculate Digit Verification of CAS Registry Number 1346547-00:
(9*1)+(8*3)+(7*4)+(6*6)+(5*5)+(4*4)+(3*7)+(2*0)+(1*0)=159
159 % 10 = 9
So 1346547-00-9 is a valid CAS Registry Number.
1346547-00-9Upstream product
1346547-00-9Downstream Products
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GSK583
