GSK 583 - ≥98%(HPLC), high purity , CAS No.1346547-00-9, Inhibitor of receptor interacting serine/threonine kinase 2

Item Number
G286537
Grouped product items
SKUSizeAvailabilityPrice Qty
G286537-5mg
5mg
In stock
$165.90
G286537-10mg
10mg
In stock
$260.90
G286537-25mg
25mg
In stock
$587.90
G286537-50mg
50mg
In stock
$890.90

Potent RIPK2 inhibitor and cell permeable

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent RIPK2 inhibitor (IC50values are 2 and 5 nM at rat and human kinases, respectively). Displays selectivity for RIP2K over p38α, VEGFR2 and a panel of 300 kinases. Exhibits some inhibition at BRK and Aurora A. Also displays similar binding affinity, b
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of receptor interacting serine/threonine kinase 2
Product Description

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.

Associated Targets(Human)

RIPK3 Tchem Receptor-interacting serine/threonine-protein kinase 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IL1R1 Tclin Interleukin-1 receptor (14 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TGFBR1 Tchem TGF-beta receptor type I (3786 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GAK Tchem Serine/threonine-protein kinase GAK (1150 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK2 Tchem Serine/threonine-protein kinase RIPK2 (1546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTK6 Tchem Tyrosine-protein kinase BRK (2605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Monocyte (474 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TLR4 Tchem Toll-like receptor 4 (970 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TLR2 Tchem Toll-like receptor 2 (975 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NOD1 Tchem Nucleotide-binding oligomerization domain-containing protein 1 (1322 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NOD2 Tclin Nucleotide-binding oligomerization domain-containing protein 2 (1613 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK3 Tchem Receptor-interacting serine/threonine-protein kinase 3 (468 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Tlr7 Toll-like receptor 7 (174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Whole blood (71 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Ripk2 Receptor-interacting serine/threonine-protein kinase 2 (6 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488202097
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488202097
IUPAC Name 6-tert-butylsulfonyl-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine
INCHI InChI=1S/C20H19FN4O2S/c1-20(2,3)28(26,27)13-5-7-16-14(11-13)17(8-9-22-16)23-19-15-10-12(21)4-6-18(15)24-25-19/h4-11H,1-3H3,(H2,22,23,24,25)
InChi Key XLOGLWKOHPIJLV-UHFFFAOYSA-N
Canonical SMILES CC(C)(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=NNC4=C3C=C(C=C4)F
Isomeric SMILES CC(C)(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=NNC4=C3C=C(C=C4)F
PubChem CID 67469084
MeSH Entry Terms 6-(tert-butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine;GSK583
Molecular Weight 398.45

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
D2301304Certificate of AnalysisFeb 06, 2023 G286537
D2301307Certificate of AnalysisFeb 06, 2023 G286537
D2301308Certificate of AnalysisFeb 06, 2023 G286537
D2301336Certificate of AnalysisFeb 06, 2023 G286537
D2301339Certificate of AnalysisFeb 06, 2023 G286537
D2301340Certificate of AnalysisFeb 06, 2023 G286537
D2301341Certificate of AnalysisFeb 06, 2023 G286537
D2301342Certificate of AnalysisFeb 06, 2023 G286537

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 39.84, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 7.97, Max Conc. mM: 20

Related Documents

References

1. Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus Jr R, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB et al..  (2016)  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..  J Med Chem,  59  (10): (4867-80).  [PMID:27109867] [10.1021/op500134e]

Solution Calculators