GSK-199 hydrochloride

Names

[ Name ]:
GSK-199 hydrochloride

[Synonym ]:
(R)-(3-Aminopiperidin-1-yl)(2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride
[(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 hydrochloride (1:1)
Methanone, [(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-, hydrochloride (1:1)

Biological Activity

[Description]:

GSK-199 hydrochloride is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.

[References]

References 1. Lewis HD, et al. Nat Chem Biol. 2015 Mar;11(3):189-91. 2. Willis VC, et al. Clin Exp Immunol. 2017 May;188(2):263-274. 3. Slade DJ, et al. ACS Chem Biol. 2015 Apr 17;10(4):1043-53. View Related Products by Target Protein Arginine Deiminase (PAD)

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₉ClN₆O₂

[ Molecular Weight ]:
468.979

[ Exact Mass ]:
468.204041

Related Compounds

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