2. Epigenetics
  3. Protein Arginine Deiminase

Protein Arginine 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 (41):

Cat. No. Product Name Effect Purity
  • HY-100574A
    Cl-amidine hydrochloride Inhibitor
    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[1][2][3][4][5].
  • 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)[1].
  • 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[1].
  • HY-111347A
    BB-Cl-Amidine hydrochloride Inhibitor 99.47%
    BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor[1].
  • HY-100514
    GSK484 hydrochloride Inhibitor
    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.
  • 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[1].
  • 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[1].
  • 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[1].
  • HY-120343
    GSK106 Inhibitor 98.00%
    GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199[1].
  • 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[1].
  • 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[1][2][3].
  • 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[1].
  • 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[1].
  • 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[1].
  • 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[1][2].
  • 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[1].
  • 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[1].
  • 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[1].
  • 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[1][2][3][4][5].
  • 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[1].