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

Protein Arginine Deiminase

Peptidylarginine Deiminase

Protein Arginine Deiminase

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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 관련 제품 (64):

Cat. No. 상품명 효과 Purity Chemical Structure
  • 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-176711
    PAD-PF1
    		Inhibitor
    PAD-PF1 is a PAD4 inhibitor (IC50: 15.9 µM). PAD-PF1 binds to an allosteric site of PAD-PF1, which is distinct from substrate and GSK147.
    PAD-PF1
  • HY-B1505G
    Acefylline (GMP)
    		Activator
    Acefylline (Theophyllineacetic acid) (GMP), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline (GMP) is a peptidylarginine deiminase (PAD) activator. Acefylline (GMP) is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline (GMP) can be used in asthma research.
    Acefylline (GMP)
  • HY-111347B
    BB-Cl-Amidine TFA
    		Inhibitor
    BB-Cl-Amidine TFA is a peptidylarginine deminase (PAD) inhibitor.
    BB-Cl-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-P11870
    PADI4_7
    		Ligand
    PADI4_7 is an inert binder of peptidylarginine deiminase IV (PADI4) with a Kd value of 8 nM. PADI4_7 binds to PADI4 but does not modulate its catalytic activity. PADI4_7 can be functionalized into a biotinylated probe (bio-PADI4_7), which enriches intracellular PADI4 from cell extracts for biochemical analyses, including the identification of PADI4-interacting proteins under resting or activated conditions.
    PADI4_7
  • 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-P11869
    PADI4_11
    		Activator
    PADI4_11 is an isoform-selective, allosteric PADI4 activator with a Kd of 457 nM. PADI4_11 enters cells via active transport, does not induce cytotoxicity or membrane damage, and serves as a tool for investigating the regulation, function and cellular reprogramming of PADI4. PADI4_11 can be used in studies related to rheumatoid arthritis and ulcerative colitis.
    PADI4_11
  • HY-176709
    GSK147
    		Inhibitor
    GSK147 is a PAD4 inhibitor with a Kd of 0.47 µM. GSK147 inhibits Ionomycin (HY-13434) induced protein citrullination in human isolated neutrophils.
    GSK147
  • 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-174349
    PAD-IN-3
    		Inhibitor
    PAD-IN-3 (Compound 16) is a potent dual peptidyl arginine deiminases 4 (PAD4) and PAD1 inhibitor with IC50 values of 0.204 μM and 0.273 μM, respectively. PAD-IN-3 is promising for research of citrullination-associated disorders such as cancer and autoimmune diseases.
    PAD-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 (Theophyllineacetic acid) (Standard) is the analytical standard of Acefylline (HY-B1505). This product is intended for research and analytical applications. 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 (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-100514R
    GSK484 hydrochloride (Standard)
    		Inhibitor
    GSK484 (hydrochloride) (Standard) is the analytical standard of GSK484 (hydrochloride) (HY-100514). This product is intended for research and analytical applications. 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 (Standard)
  • 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