A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils

GSK484 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1652591-81-5
Storage:
-20
UN-No:
Non-Hazardous - /

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils

Formal name: [(3S,4R)-3-amino-4-hydroxy-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-indol-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride

Synonyms: 

Molecular weight: 510

CAS: 1652591-81-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deiminases||Research Area|Epigenetics, Transcription, & Translation|Writers|Citrullination||Research Area|Immunology & Inflammation|Innate Immunity|NETosis

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