GSK484

GSK484

Stock Code: 3575229
Manufacturer Part No: SML1658-25MG
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Biochem/physiol Actions


GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC50 values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1–11 even at 100 µM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a β-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc


Features and Benefits


GSK484 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.


This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.


Other Notes


GSK484 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK484 probe summary on the Chemical Probes Portal website.


Packaging


5, 25 mg in glass bottle

Colourwhite to beige
Quality Level100
InChI keyMULKOGJHUZTANI-ADMBKAPUSA-N
InChI1S/C27H31N5O3.ClH/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16;/h3-6,11-13,16,19,23,33H,7
ManufacturerSIGMA-ALDRICH
SolubilityH2O: 2 mg/mL, clear (warmed)
Formpowder
Assay≥98% (HPLC)

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