Protein Arginine Deiminase
Peptidylarginine 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.
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Protein Arginine Deiminase Related Products (66)
Related Products (66)
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Acefylline (GMP)
0 ImagesSynonyms: Theophyllineacetic acid (GMP); Theophylline-7-acetic acid (GMP)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.
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BB-Cl-Amidine TFA
0 ImagesCat. No.: HY-111347BBB-Cl-Amidine TFA is a peptidylarginine deminase (PAD) inhibitor.
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PF-3166
0 ImagesCat. No.: HY-169206CAS No.: 3126204-69-8PF-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)..
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PAD3-IN-1
0 ImagesCat. No.: HY-139088CAS No.: 1671088-84-8PAD3-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.
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PAD4-IN-4
0 ImagesCat. No.: HY-162494CAS No.: 3044006-76-7PAD4-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.
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PADI4_7
0 ImagesCat. No.: HY-P11870PADI4_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.
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Anti-PAD4 Antibody
0 ImagesCat. No.: HY-P992287
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Histone H4 peptide substrate (1-21)
0 ImagesCat. No.: HY-P11724CAS No.: 374899-66-8Histone H4 peptide substrate (1-21) is a PAD4 peptide substrate. Histone H4 peptide substrate (1-21) serves as a substrate for the PAD4-catalyzed hydrolytic deimination of arginine residues, producing citrulline and ammonia.
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PADI4_11
0 ImagesCat. No.: HY-P11869PADI4_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.
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GSK147
0 ImagesCat. No.: HY-176709CAS No.: 1550371-16-8
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PAD4-IN-3
0 ImagesCat. No.: HY-157157CAS No.: 2642327-44-2PAD4-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.
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BB-Cl-Amidine (Standard)
0 ImagesCat. No.: HY-111347RCAS No.: 1802637-39-3BB-Cl-Amidine (Standard) is the analytical standard of BB-Cl-Amidine (HY-111347). This product is intended for research and analytical applications. BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
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PAD2-IN-2 TFA
0 ImagesCat. No.: HY-171002APAD2-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.
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Acefylline (Standard)
0 ImagesSynonyms: Theophyllineacetic acid (Standard); Theophylline-7-acetic acid (Standard)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.
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YW3-56 hydrochloride
0 ImagesYW3-56 (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.
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BB-F-Yne
0 ImagesCat. No.: HY-137124CAS No.: 2219331-30-1BB-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.
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GSK484 hydrochloride (Standard)
0 ImagesGSK484 (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.
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PAD2-IN-2
0 ImagesCat. No.: HY-171002PAD2-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.
