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 (64):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-42034
    Hydroquinine
    		Inhibitor 99.87%
    Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride.
    Hydroquinine
  • 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 reverses physical disability in the EAE mouse model of multiple sclerosis (MS) and eliminates T cell infiltration in the brain. KP-302 can be studied in research as a disease-modifying agent for MS.
    KP-302
  • HY-176710
    PAD-PF2
    		Inhibitor 99.94%
    PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer.
    PAD-PF2
  • 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-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-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-137125
    BB-Cl-Yne
    		Inhibitor 98.14%
    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-P992098
    Adargiminase
    Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer.
    Adargiminase
  • HY-100574B
    Cl-amidine TFA
    		Inhibitor 98.10%
    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-P1417
    TDFA
    		Inhibitor
    TDFA is an irreversible inhibitor of protein arginine deiminase 4 (PAD4).
    TDFA
  • HY-W297348
    (Rac)-Cl-amidine
    (Rac)-Cl-amidine is an orally active peptidyl arginine deimidase (PAD) inhibitor with the property of inhibiting PAD activity. (Rac)-Cl-amidine exhibits enhanced efficacy in cells and can be used to study PAD function. (Rac)-Cl-amidine can effectively regulate gene transcription, cell differentiation and innate immune response.
    (Rac)-Cl-amidine
  • HY-132286
    2-PADQZ
    2-PADQZ is an antiviral compound with activity against influenza viruses. 2-PADQZ specifically binds to the influenza A virus RNA promoter and forms a binding site at the internal loop. 2-PADQZ has a significant inhibitory effect on H1N1 and H3N2 influenza A viruses and influenza B viruses.
    2-PADQZ
  • HY-173321
    PAD4-IN-5
    		Inhibitor
    PAD4-IN-5 (Example 18) is a PAD4 inhibitor with IC50s of ≤10 nM and 101-500 nM for human PAD4 (hPAD4) under 50 µM Ca2+ and 1 mM Ca2+ conditions, respectively. PAD4-IN-5 can be used for the study of autoimmune disease, such as rheumatoid arthritis (RA).
    PAD4-IN-5
  • HY-175518
    PADI4-IN-1
    		Inhibitor
    PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC50 of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis.
    PADI4-IN-1
  • HY-175258
    PAD2/4-IN-1
    		Inhibitor
    PAD2/4-IN-1 (Compound 4f) is an orally active inhibitor of PAD2 and PAD4 with IC50 values of 23 nM and 10 nM, respectively. PAD2/4-IN-1 can inhibit protein citrullination in neutrophils and reduce hERG channel liabilities. PAD2/4-IN-1 can be used in the research of autoimmune diseases, neurological disorders, and cancers.
    PAD2/4-IN-1
  • HY-178365
    PAD-IN-4
    		Inhibitor
    PAD-IN-4 is a potent PAD inhibitor (PAD 1/4, IC50 = 0.273/0.24 μM). PAD-IN-4 shows no significant cytotoxicity against A549 or MDA-MB-231 cells. PAD-IN-4 can be used for the study of cancer and autoimmune diseases.
    PAD-IN-4