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-100574
    Cl-amidine
    		Inhibitor
    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.
    Cl-amidine
  • HY-155052
    PAD4-IN-2
    		Inhibitor
    PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils.
    PAD4-IN-2
  • HY-100574B
    Cl-amidine TFA
    		Inhibitor
    Cl-amidine TFA 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 TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
    Cl-amidine TFA
  • HY-100574C
    D-Cl-amidine
    		Inhibitor
    D-Cl-amidine is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.
    D-Cl-amidine
  • HY-137655
    BMS-P5
    		Inhibitor
    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.
    BMS-P5
  • HY-126560A
    F-Amidine TFA
    		Inhibitor
    F-Amidine TFA is a Protein arginine deiminase 4 (PAD4) inhibitor. F-Amidine TFA can be used in the study of inflammatory and immune system diseases (such as rheumatoid arthritis).
    F-Amidine TFA
  • HY-157157
    PAD4-IN-3
    		Inhibitor
    PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment.
    PAD4-IN-3
  • HY-150307
    KP-302
    		Inhibitor
    KP-302 (compound 23) is a selective inhibitor of protein arginine deaminase PAD2 with a Ki of 60 μM. KP-302 also reversed physical disability in the EAE mouse model of multiple sclerosis (MS) and eliminated T cell infiltration in the brain. KP-302 has the potential to be a disease-modifying agent for MS.
    KP-302
  • HY-B1505R
    Acefylline (Standard)
    		Activator
    Acefylline (Standard) is the analytical standard of Acefylline. This product is intended for research and analytical applications. 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 (Standard)
  • HY-124586A
    (rac)-Streptonigrin
    		Inhibitor
    (rac)-Streptonigrin ((rac)-Bruneomycin) is the racemic form of Streptonigrin. Streptonigrin (HY-124586) is a natural product produced by the actinobacterium Streptomyces flocculus, exhibiting antitumor and antibacterial activities. Streptonigrin can act as a pan-PAD inhibitor, with IC50 values of 48.3 μM, 26.1 μM, 0.43 μM, and 2.5 μM for PAD1, PAD2, PAD3, and PAD4, respectively.
    (rac)-Streptonigrin
  • HY-137124
    BB-F-Yne
    		Inhibitor
    BB-F-Yne is a protein arginine deiminase (PAD) inhibitor with Ki values of PAD1-4.are 2050, 1700, 1100, 3100 M-1min-1 respectively. BB-F-Yne can be used as a click probe to label PAD.
    BB-F-Yne
  • HY-126560
    F-Amidine
    		Inhibitor
    F-Amidine is a Protein arginine deiminase 4 (PAD4) inhibitor. F-Amidine can be used in the study of inflammatory and immune system diseases (such as rheumatoid arthritis).
    F-Amidine
  • HY-B1505A
    Acefylline piperazine
    		Activator
    Acefylline piperazine, a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline piperazine is a peptidylarginine deiminase (PAD) activator. Acefylline piperazine is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline piperazine can be used in asthma research.
    Acefylline piperazine
  • HY-115676
    GSK199 analog hydrochloride
    		Inhibitor
    GSK199 analog hydrochloride belongs to a class of compounds that inhibit PAD4 (guanidinoarginine deiminase 4). GSK199 analog hydrochloride has potential uses in diseases including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosus, and psoriasis.
    GSK199 analog hydrochloride