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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PAD4-IN-2 TFA
0 ImagesCat. No.: HY-155052APAD4-IN-2 TFA is a highly tumor-targeted and irreversible PAD4 inhibitor with an IC50 of 1.94 μM. PAD4-IN-2 TFA selectively recognizes sialic acid on tumor surfaces and accumulates in tumor tissues, with distribution in the cytoplasm of tumor cells and nuclei of neutrophils. PAD4-IN-2 TFA inhibits the PAD4-H3cit-NETs (Neutrophil Extracellular Traps) pathway, reduces senescent tumor-associated neutrophils, and promotes M1 macrophage polarization. The compound exhibits potent anti-tumor and anti-metastatic activities and is suitable for breast cancer research.
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KP-302
0 ImagesKP-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.
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PAD-PF2
0 ImagesCat. No.: HY-176710Purity: 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.
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AFM-30a
0 ImagesCat. No.: HY-125099CAS No.: 2095107-57-4AFM-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.
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DFPM
0 ImagesDFPM 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.
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AFM32a
0 ImagesCat. No.: HY-136557CAS No.: 2095109-82-1Synonyms: PAD2-IN-1AFM32a (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).
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Cl-amidine
0 ImagesCat. No.: HY-100574CAS No.: 913723-61-2Cl-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.
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PAD4-IN-2
0 ImagesCat. No.: HY-155052CAS No.: 2642327-52-2PAD4-IN-2 is a highly tumor-targeted and irreversible PAD4 inhibitor with an IC50 of 1.94 μM. It selectively recognizes sialic acid on tumor surfaces and accumulates in tumor tissues, with distribution in the cytoplasm of tumor cells and nuclei of neutrophils. PAD4-IN-2 inhibits the PAD4-H3cit-NETs (Neutrophil Extracellular Traps) pathway, reduces senescent tumor-associated neutrophils, and promotes M1 macrophage polarization. The compound exhibits potent anti-tumor and anti-metastatic activities and is suitable for breast cancer research.
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BB-Cl-Yne
0 ImagesCat. No.: HY-137125CAS No.: 2219324-71-5BB-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.
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Cl-amidine TFA
0 ImagesCl-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.
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D-Cl-amidine
0 ImagesCat. No.: HY-100574CCAS No.: 1404060-15-6D-Cl-amidine is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.
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TDFA
0 ImagesCat. No.: HY-P1417CAS No.: 1345019-64-8Synonyms: Thr-Asp-F-amidineTDFA is an irreversible inhibitor of protein arginine deiminase 4 (PAD4).
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(Rac)-Cl-amidine
0 ImagesCat. No.: HY-W297348CAS No.: 1965308-76-2(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.
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2-PADQZ
0 ImagesCat. No.: HY-132286CAS No.: 60547-97-92-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.
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PAD4-IN-5
0 ImagesCat. No.: HY-173321CAS No.: 3071873-52-1PAD4-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).
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PADI4-IN-1
0 ImagesCat. No.: HY-175518PADI4-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.
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PAD2/4-IN-1
0 ImagesCat. No.: HY-175258CAS No.: 3105974-36-2PAD2/4-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.
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F-Amidine TFA
0 ImagesCat. No.: HY-126560ACAS No.: 877617-46-4F-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).
