The initial compound identified in a screen for PAD4 inhibitors (IC50 = 3.2 µM in functional assay) that was optimized to produce the more potent PAD4 inhibitors

GSK121 (trifluoroacetate salt) – 1 mg

Brand:
Cayman
CAS:
1652591-80-4
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} GSK121 is the initial compound identified in a screen for PAD4 inhibitors and was optimized to produce the more potent PAD4 inhibitors, GSK484 (Item No. 17488) and GSK199 (Item No. 17489).{28376} GSK121 was shown to inhibit the citrullination of PAD4 target proteins in a functional assay with an IC50 value of 3.2 µM.{28376}  

 

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Description

The initial compound identified in a screen for PAD4 inhibitors (IC50 = 3.2 µM in functional assay) that was optimized to produce the more potent PAD4 inhibitors, GSK484 and GSK199

Formal name: (3-​amino-1-​piperidinyl)​[1-​methyl-​2-​(1-​methyl-​1H-​indol-​2-​yl)​-​1H-​benzimidazol-​5-​yl]​-methanone, 2,​2,​2-​trifluoroacetate

Synonyms: 

Molecular weight: 501.5

CAS: 1652591-80-4

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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