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 (41):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-150307
    KP-302
    		Inhibitor 99.78%
    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-119994
    DFPM
    		99.4%
    DFPM activates plant resistance protein signaling in roots, and triggers root growth arrest. DFPM decreases root cell viability in accession Col-0. DFPM is light sensitive in aqueous solutions. DFPM becomes bioactive during light and oxygen-dependent modification.
    DFPM
  • 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
  • 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-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-139088
    PAD3-IN-1
    PAD3-IN-1 (compound 14b) is an inhibitor of protein arginine deiminase (PAD) and is more than 10-fold more selective for PAD3 than PAD 1, 2, and 4. The IC50 values ​​of PAD3-IN-1 for PAD 1, 2, 3, and 4 are 120, 27.5, 4.5, and 30.5 μM, respectively. And PAD3 is a PAD isoform associated with neurodegenerative responses to spinal cord injury, and PAD3-IN-1 could be used to study PAD-related neurological diseases.
    PAD3-IN-1
  • 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-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-171002A
    PAD2-IN-2 TFA
    		Inhibitor
    PAD2-IN-2 (cis-isomer of 1) TFA is a protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-2 TFA possess an azobenzene photoswitch to optically control PAD activity. PAD2-IN-2 TFA inhibits histone H3-citrullination.
    PAD2-IN-2 TFA
  • 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-112903A
    YW3-56 hydrochloride
    		Inhibitor
    YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer.
    YW3-56 hydrochloride
  • 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-169206
    PF-3166
    		Inhibitor
    PF-3166 is a PAD2 inhibitor (IC50=150 nM) that is competitive with Ca2+. TPF-3166 insignificantly inhibits PAD3 or PAD4 (80 μM). PF-3166 also inhibits NH3 release (IC50=580 nM)..
    PF-3166
  • HY-171002
    PAD2-IN-2
    		Inhibitor
    PAD2-IN-2 (cis-isomer of 1) is a protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-2 possess an azobenzene photoswitch to optically control PAD activity. PAD2-IN-2 inhibits histone H3-citrullination.
    PAD2-IN-2
  • 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