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PAD

In enzymology, a protein-arginine deiminase is an enzyme that catalyzes a form of post translational modification called arginine de-imination or citrullination. 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.

  • Cl-amidine hydrochloride
    T10831L1373232-26-8
    Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.
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  • BMS-P5
    T222771549811-36-0
    BMS-P5 is a specific and orally active Peptidylarginine Deiminase 4 (PAD4) inhibitor.
    • $148
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  • N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide
    T98281965308-76-2In house
    N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide is a racemic form of Cl-amidine (S enantiomer). Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor.
    • $50
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  • Bongkrekic acid
    T3606711076-19-0
    Bongkrekic acid (Bongkrekic Acid (ammonium salt)) is a mitochondrial toxin secreted by Burkholderia gladioli that inhibits adenine nucleotide translocase (ANT).Bongkrekic acid Bongkrekic acid Bongkrekic acid induces extracellular traps in neutrophils through signaling mediated by p38, ERK, PAD4, and P2X1.
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  • GSK484 hydrochloride
    TQ00671652591-81-5
    GSK484 hydrochloride (GTPL8577) (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor. It demonstrates high-affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.
    • $68
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  • BB-Cl-Amidine
    T104821802637-39-3
    BB-Cl-Amidine is an inhibitor of peptidyl arginine deminase (PAD).
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  • BMS-P5 free base
    T22277L1550371-22-6
    BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma.
    • $82
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  • GSK199
    T88611549811-53-1
    GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).
    • $98
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  • Acefylline
    T2205652-37-9
    Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects
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  • GSK121
    T241051652591-80-4
    GSK121 is an inhibitor of selective PAD4.
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