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GSK484 hydrochloride 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.
| Molecular Weight | 510.03 |
| Formula | C27H31N5O3.HCl |
| CAS Number | 1652591-81-5 |
| Solubility (25°C) | DMSO 100 mg/mL Water 50 mg/mL |
| Storage | 2-8°C, dry, sealed |
| Related PAD Products |
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| Streptonigrin
Streptonigrin (Bruneomycin), a natural product produced by Streptomyces flocculus, acts as a pan-PAD inhibitor with IC50s of 48.3±34.2 µM, 26.1±0.3 µM, 0.43±0.03 µM, and 2.5±0.4 µM for PAD1, PAD2, PAD3, and PAD4, respectively. Streptonigrin possesses both anti-tumor and anti-bacterial activity. |
| PAD4-IN-2
PAD4-IN-2 is a PAD4 inhibitor (IC50=1.94 μM). |
| Cl-amidine
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model. |
| GSK106
GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199. |
| BMS-P5 free base
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model. |
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