GSK583

SKU: orb1304095

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Description

GSK583 is a potent and selective inhibitor of RIP2 kinase, exhibiting an IC50 of 5 nM. This compound is a valuable research tool for studying the NOD signaling pathway in both cellular and animal models of inflammatory and autoimmune diseases.

Research Area

Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	1346547-00-9
MW	398.4
Purity	>98%
Formula	C₂₀H₁₉FN₄O₂S
SMILES	CC(C)(C)S(=O)(=O)c1ccc2nccc(Nc3n[nH]c4ccc(F)cc34)c2c1
Target	Kinase
Solubility	Soluble in DMSO (up to 25 mg/ml)

Bioactivity

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Target IC50	RIP2:5 nM
In Vivo	GSK583 has moderate volumes of distribution, low clearance, and moderate oral bioavailability (in rat and mouse). Although GSK583 would not produce a human pharmacodynamic response within an acceptable dose range, the oral PK in mouse and rat supplies enough systemic exposure for use as a preclinical in vivo tool molecule in an acute inflammation challenge model. Read more...
In Vitro	GSK583 possesses a comparable binding affinity for RIP3 kinase similarly to the RIP2 (RIP2/3 FP IC50: 5/16 nM) by an in-house FP binding assay configured. But GSK583 (10 μM) shows little or no inhibition of RIP3-dependent necroptotic cell death in a cellular assay. GSK583 effectively and dose-dependently inhibits MDP-stimulated TNFα production (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 cytokine receptors (IL-1R, TNFR) or Toll-like receptors (TLR2, TLR4, TLR7) but complete inhibition is observed upon activation of NOD1/2 receptors, which signal in a RIP2-dependent manner. Although it has excellent kinase selectivity, GSK583 does inhibit both the hERG channel and CYP3A4. Read more...
Cell Research	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. (Only for Reference) Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, GSK 583, GSK583, GSK-583, inhibit, RIP3, RIP kinase, RIP1, RIPkinase, RIPK, Receptor-interacting protein kinases

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Compound Identifiers

PubChem CID

67469084 ↗

Key Properties

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No computed properties available.

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GSK583 (orb1304095)

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Purity:	>98% (HPLC)
CAS Number:	1346547-00-9
MW:	398.4539
Formula:	C₂₀H₁₉FN₄O₂S

GSK583

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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