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GSK-199 hydrochloride

Chemical Structure : GSK-199 hydrochloride

CAS No.: 1549811-53-1

GSK-199 hydrochloride (GSK199)

Catalog No.: PC-62217Not For Human Use, Lab Use Only.

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.

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Biological Activity

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.
GSK-199 shows high specificity for PAD4 over PAD1/2/3/6.
GSK-199 affects cellular citrullination and mimic the deficiency in NET production in mice.
GSK-199 significantly decreases in complement C3 deposition in both synovium and cartilage in mice.
GSK199 also inhibits human beta-coronaviruse HCoV-OC43 replication.

Physicochemical Properties

M.Wt 468.986
Formula C24H29ClN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[(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

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.

4. Selina Pasquero, et al. Antiviral Res. 2022 Mar 11;200:105278.

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