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GSK484

Chemical Structure : GSK484

CAS No.: 1652629-23-6

GSK484 (GSK-484)

Catalog No.: PC-62214Not For Human Use, Lab Use Only.

GSK484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.
GSK484 shows high specificity for PAD4 over PAD1/2/3/6.
GSK484 causes a clear, statistically-significant reduction in diffused NETs.

Physicochemical Properties

M.Wt 473.577
Formula C27H31N5O3
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

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

References

1. Lewis HD, et al. Nat Chem Biol. 2015 Mar;11(3):189-91.

2. Cedervall J, et al. Oncoimmunology. 2017 Apr 20;6(8):e1320009.

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