A selective inhibitor of PAD4 (IC50 = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils

GSK199 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1549811-53-1
Storage:
-20
UN-No:
Non-Hazardous - /

Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases.{18134} GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.{28376}It is less potent than the related PAD4 inhibitor GSK484 (Item No. 17488), which demonstrates an IC50 value of 50 nM.{28376} GSK199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.{28376}  

 

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Description

A selective inhibitor of PAD4 (IC50 = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils

Formal name: [(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride

Synonyms: 

Molecular weight: 469

CAS: 1549811-53-1

Purity: ≥98%

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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