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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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| Cl-amidine hydrochloride
Cl-amidine hydrochloride 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. |
| GSK199 hydrochloride
GSK199 hydrochloride is a selective PAD4 inhibitor with half-maximum inhibitory concentration (IC50) values, in the absence of calcium, of 200 nM. |
| GSK-121 Trifluoroacetate
GSK-121 Trifluoroacetate is a selective inhibitor of PAD4. |
| BB-Cl-Amidine
BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor. |
| BMS-P5
BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model. |
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