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You are here:Home-Inhibitors & Agonists-Metabolic Enzyme/Protease-Protein Arginine Deiminase (PAD)

Request The Product List ofProtein Arginine Deiminase (PAD) Protein Arginine Deiminase (PAD)

Protein arginine deiminases (PADs) is a unique family of enzymes that catalyzes the hydrolysis of peptidyl-arginine to form peptidyl-citrulline on histones, fibrinogen, and other biologically relevant proteins. In humans, the PAD family is composed of five, calcium dependent isozymes (PADs 1-4 and 6), which share roughly 50% sequence similarity. PADs are found in a myriad of cell and tissue types, including the epidermis and uterus (PAD1), skeletal muscle, brain, inflammatory cells, several cancer cell lines, and secretory glands (PAD2), hair follicles and keratinocytes (PAD3), granulocytes and several types of cancer (PAD4), and oocytes and embryos (PAD6). PAD4, the best characterized isozyme, has also been shown to citrullinate a number of other proteins, including p300, ING4, RPS2, lamin C, and nucleophosmin.

Cat. No. Product Name CAS No. Information
H5469

GSK-484 hydrochloride

 		1652591-81-5

GSK-484 hydrochloride 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; shows high specificity for PAD4 over PAD1/2/3/6; causes a clear, statistically-significant reduction in diffused NETs.
H5468

GSK-484

 		1652629-23-6

GSK-484 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; shows high specificity for PAD4 over PAD1/2/3/6; causes a clear, statistically-significant reduction in diffused NETs.
H5467

GSK-199 hydrochloride

 		1549811-53-1

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; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.
H5466

GSK-199

 		1549810-81-2

GSK-199 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; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.
H5472

YW3-56

 		1374311-17-7

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor with inhibitory activity against PAD2 (IC50=0.5-1 uM) and PAD4 (IC50=1-2 uM), inhibits U2OS cancer cell growth with IC50 of 2.5 uM; activates a cohort of p53 target genes, including SESN2, which in turn inhibits the mTORC1 signaling pathway, thereby perturbing autophagy and inhibiting cancerous cell growth, effectively inhibits the growth of triple-negative breast cancer xenograft tumors in nude mice; also significantly blocks LPS-induced pulmonary vascular leakage, alleviates acute lung injury, and improves survival in mouse model of lethal LPS-induced endotoxemia.
H5471

Thr-Asp-F-amidine

 		1345019-64-8

Thr-Asp-F-amidine (TDFA) is a highly potent, selective PAD4 (protein arginine deiminase 4) inhibitor with IC50 of 2.3 uM, displays ≥15-fold selectivity for PAD4 versus PAD1 and ≥50-fold versus PADs 2 and 3; active in cells and can be used to inhibit PAD4 activity in cellulo.
H5470

Streptonigrin

 		3930-19-6

Streptonigrin (Bruneomycin, NSC 45383) is a potent, selective, and irreversible PAD4 inactivator with IC50 of 1.87 uM, also binds directly to RAD54 with Kd of 9.1 uM, inhibits ATPase and DNA branch migration activity of RAD54; inhibits branch migration of model Holliday junctions with IC50 of 16.5 uM, inhibits ATP hydrolysis with IC50 of 14.4 uM, also binds and inhibits the SUMO-specific protease SENP1.

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