2. Signaling Pathways
  3. Epigenetics
  4. Protein Arginine Deiminase

Protein Arginine Deiminase

Peptidylarginine Deiminase

Protein Arginine Deiminase

Related Products

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Protein arginine deiminase (PAD), is a group of calcium-dependent enzymes, which play crucial roles in citrullination, and can catalyze arginine residues into citrulline. his chemical reaction induces citrullinated proteins formation with altered structure and function, leading to numerous pathological diseases, including inflammation and autoimmune diseases. These pathologies established the PADs as therapeutic targets and multiple PAD inhibitors are known.

Humans encode five PADs, designated PADs 1-4 and PAD6. Of the five PAD isozymes (PAD1, 2, 3, 4 and 6), only four (PADs1-4) are catalytically active. PAD activity is tightly regulated by Ca2+ and PADs contain 4 (PAD1), 5 (PAD3, 4) or 6 (PAD2) Ca2+-binding sites. Dysregulated PAD activity, most notably PAD2 and PAD4, is associated with multiple inflammatory diseases (e.g., rheumatoid arthritis) as well as cancer, and PAD inhibitors, such as Cl-amidine and BB-Cl-amidine, show efficacy in multiple preclinical animal models of disease.

Protein Arginine Deiminase Related Products (34):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100514
    GSK484 hydrochloride
    		Inhibitor 99.72%
    GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.
    GSK484 hydrochloride
  • HY-100574A
    Cl-amidine hydrochloride
    		Inhibitor 99.39%
    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. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
    Cl-amidine hydrochloride
  • HY-111347A
    BB-Cl-Amidine hydrochloride
    		Inhibitor 99.47%
    BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor.
    BB-Cl-Amidine hydrochloride
  • HY-125099A
    AFM-30a hydrochloride
    		Inhibitor 99.96%
    AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a hydrochloride can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis.
    AFM-30a hydrochloride
  • HY-136557A
    AFM32a hydrochloride
    		Inhibitor 99.71%
    AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).
    AFM32a hydrochloride
  • HY-155052A
    PAD4-IN-2 TFA
    		Inhibitor
    PAD4-IN-2 (compound 5i) TFA is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 TFA inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils.
    PAD4-IN-2 TFA
  • HY-162494
    PAD4-IN-4
    		Inhibitor
    PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research.
    PAD4-IN-4
  • HY-137125
    BB-Cl-Yne
    		Inhibitor
    BB-Cl-Yne is a protein arginine deiminase (PAD) inhibitor with Ki values of PAD1-4.are 6400, 3600, 10800, 4900 M-1min-1 respectively. BB-Cl-Yne can be used as a click probe to label PAD.
    BB-Cl-Yne
  • HY-103058
    GSK199
    		Inhibitor 99.86%
    GSK199 is an orally active, reversible, and selective PAD4 inhibitor with an IC50 of 200 nM in the absence of calcium. GSK199 can be used for the research of rheumatoid arthritis.
    GSK199
  • HY-100574D
    D-Cl-amidine hydrochloride
    		Inhibitor 99.91%
    D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.
    D-Cl-amidine hydrochloride
  • HY-137655A
    BMS-P5 free base
    		Inhibitor 99.96%
    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.
    BMS-P5 free base
  • HY-135304
    PAD-IN-2
    		Inhibitor 99.02%
    PAD-IN-2 is a potent pad4 inhibitor (IC50: <1 μM). PAD-IN-2 can be used in the research of auto-immune diseases and cancers, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
    PAD-IN-2
  • HY-117777
    GSK121
    		Inhibitor 99.81%
    GSK-121 Trifluoroacetates a selective PAD4 inhibitor.
    GSK121
  • HY-124586
    Streptonigrin
    		Inhibitor 99.20%
    Streptonigrin (Bruneomycin), a natural product produced by Streptomyces flocculus, possesses both anti-tumor and anti-bacterial activity. Streptonigrin 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
  • HY-153450
    JBI-589
    		Inhibitor 98.93%
    JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research.
    JBI-589
  • HY-B1505
    Acefylline
    		Activator 99.96%
    Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline
  • HY-120343
    GSK106
    		Inhibitor 98.00%
    GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199.
    GSK106
  • HY-111347
    BB-Cl-Amidine
    		Inhibitor
    BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
    BB-Cl-Amidine
  • HY-125099
    AFM-30a
    		Inhibitor
    AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis.
    AFM-30a
  • HY-136557
    AFM32a
    		Inhibitor
    AFM32a (PAD2-IN-1), a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).
    AFM32a