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

Protein Arginine Deiminase

Peptidylarginine Deiminase

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 (61):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100514
    GSK484 hydrochloride
    Inhibitor 99.48%
    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 99.82%
    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 99.83%
    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-123606
    GSK484
    Inhibitor 99.14%
    GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8+ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions.
    GSK484
  • HY-181449
    CAY10729
    Inhibitor
    CAY10729 (Compound 21) is a selective PAD2 inhibitor. CAY10729 inhibits neutrophil extracellular trap formation.
    CAY10729
  • HY-E70954
    Peptidyl Arginine Deiminase, Rabbit
    Peptidyl Arginine Deiminase, Rabbit (EC 3.5.3.15) is the enzyme that converts arginine into citrulline. Calcium is required for peptidylarginine deiminase activity in vitro.
    Peptidyl Arginine Deiminase, Rabbit
  • HY-P992287
    Anti-PAD4 Antibody
    Anti-PAD4 Antibody is a monoclonal antibody that targets PAD4. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-PAD4 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-PAD4 Antibody
  • HY-136557A
    AFM32a hydrochloride
    Inhibitor 99.37%
    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-111347
    BB-Cl-Amidine
    Inhibitor 98.19%
    BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
    BB-Cl-Amidine
  • HY-103058
    GSK199
    Inhibitor 99.85%
    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-124586
    Streptonigrin
    Inhibitor 99.20%
    Streptonigrin (Bruneomycin) is an orally active antibiotic and pan-PAD inhibitor, inhibiting PAD1, PAD2, PAD3 and PAD4 with IC50 of 48.3 μM, 26.1 μM, 0.43 μM and 2.5 μM, respectively. Streptonigrin inhibits SENP1 (IC50 of 0.518 μM) and reduces HIF1α. Streptonigrin increases p53 and Apoptosis. Streptonigrin shows antiviral activity against Rauscher murine leukemia virus. Streptonigrin has immunosuppressive effects. Streptonigrin has antitumor activity against osteosarcoma.
    Streptonigrin
  • HY-153450
    JBI-589
    Inhibitor 99.75%
    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-100574D
    D-Cl-amidine hydrochloride
    Inhibitor 99.60%
    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 99.93%
    BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model.
    BMS-P5 free base
  • HY-137655
    BMS-P5
    Inhibitor 99.23%
    BMS-P5 is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model.
    BMS-P5
  • HY-117777
    GSK121
    Inhibitor 99.81%
    GSK121 is a selective PAD4 inhibitor. GSK121 can be used in the research of PAD4-related diseases, including those characterized by abnormal NET levels and various tumors.
    GSK121
  • HY-B1505
    Acefylline
    Activator 99.52%
    Acefylline (Theophyllineacetic acid), 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-135304
    PAD-IN-2
    Inhibitor 99.29%
    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-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