Protein Arginine Deiminase (PAD)

Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

GSK484 hydrochloride (GTPL8577) is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor.

Streptonigrin (Bruneomycin), a natural product produced by Streptomyces flocculus, possesses both anti-tumor and anti-bacterial activity. Streptonigrin acts as a pan-PAD inhibitor with IC50s of 48.3??34.2 ?M, 26.1??0.3 ?M, 0.43??0.03 ?M, and 2.5??0.4 ?M for PAD1, PAD2, PAD3, and PAD4, respectively.

BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4.

Cl-amidine (hydrochloride) is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

GSK106 is a negative control compound that can be used in binding and functional assays for PAD4 inhibitors.

GSK121 trifluoroacetate is a selective inhibitor of PAD4.

GSK199 is a selective inhibitor of PAD4 with IC50 of 200 nM in the absence of calcium.

Cl-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.

D-Cl-amidine is a selective inhibitor of the peptidylarginine deiminase 1 (PAD1) enzyme. It exhibits significant biological activity in modulating citrullination processes involved in various physiological and pathological conditions. This reagent is primarily utilized in research applications focusing on inflammatory diseases, neurodegeneration, and cancer biology, providing essential insights into the role of PAD1 in cellular functions. D-Cl-amidine demonstrates a favorable toxicity profile, supporting its use in experimental settings.

D-Cl-amidine hydrochloride is a potent and selective inhibitor of protein arginine deiminase 1 (PAD1). This compound effectively modulates citrullination, a post-translational modification involved in various biological processes, including inflammation and autoimmunity. D-Cl-amidine hydrochloride is a valuable tool for research into the roles of PAD1 in disease mechanisms and therapeutic interventions. Its favorable toxicity profile enhances its utility in biochemical and cellular assays.

YW3-56 hydrochloride is a potent inhibitor of peptidylarginine deiminases (PADs). It is known to activate p53 target genes and modulate the ATF pathway, effectively blocking autophagic flux. Additionally, YW3-56 induces endoplasmic reticulum (ER) stress through the PERK-eIF2α-ATF4 signaling cascade while inhibiting the mTOR pathway. This compound has demonstrated potential in the treatment of triple-negative breast cancer, making it a valuable reagent for cancer research and therapeutic studies.

Citrulline-specific probe-rhodamine hydrate is a fluorescence-based probe targeting citrulline, a metabolite produced from arginine by protein arginine deiminases (PADs). Increased PAD activity is associated with various diseases, resulting in elevated citrulline levels. This probe enables the detection of abnormal PAD activity and can be effectively utilized in animal models, particularly in studies of ulcerative colitis, aiding in the exploration of disease mechanisms and potential therapeutic targets.

BB-Cl-Amidine hydrochloride is a selective peptidylarginine deiminase (PAD) inhibitor. It demonstrates significant inhibitory activity against PAD enzymes, influencing protein citrullination processes. This compound is utilized in research focused on the role of PAD enzymes in various diseases, such as rheumatoid arthritis and neurodegenerative disorders, as well as for exploring mechanisms of protein modification.

AFM32a hydrochloride is a selective inhibitor of protein arginine deiminase 2 (PAD2), derived from a benzimidazole structure. It demonstrates high potency and a remarkable selectivity profile, exhibiting a 95-fold preference for PAD2 over PAD4 and a 79-fold preference over PAD3. This compound is valuable for research applications focusing on the regulatory mechanisms of PAD2 in various biological processes.

GSK484 is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), effectively blocking the enzyme's catalytic activity to inhibit protein citrullination and neutrophil extracellular trap (NET) formation. This compound demonstrates anti-inflammatory properties by reducing histone H3 production, modulating MHC-I expression, and inhibiting CD8+ T cell activation and proliferation. Research applications include studies on rheumatoid arthritis, sickle cell disease, myocardial ischemia-reperfusion injury, and colitis, as well as investigations into intestinal microbial homeostasis and ferroptosis-related dysbiosis.

JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research.

BMS-P5 free base is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), demonstrating an IC50 of 98 nM. This compound exhibits specificity for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base effectively inhibits multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and has been shown to delay the progression of MM in syngeneic mouse models, making it a valuable tool for research in cancer and inflammation.

BMS-P5 is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), demonstrating an IC50 of 98 nM. This compound exhibits notable selectivity for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 effectively inhibits neutrophil extracellular trap (NET) formation induced by multiple myeloma (MM) and has been shown to delay the progression of MM in syngeneic mouse models, making it a valuable tool for research in cancer biology and the study of inflammatory responses.

PAD-IN-2 is a potent inhibitor of pad4 with an IC50 of less than 1 μM. This compound is valuable in the investigation of various autoimmune diseases and cancers, including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis, and psoriasis. Its ability to modulate pad4 activity makes it a significant tool for research aimed at understanding these complex conditions.

KP-302 is a selective inhibitor of protein arginine deiminase PAD2, exhibiting a Ki value of 60 μM. This compound demonstrates significant biological activity by reversing physical disability in the experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis (MS), as well as reducing T cell infiltration in the central nervous system. KP-302 serves as a valuable research tool for investigating disease-modifying therapies in the context of MS.

DFPM is a plant resistance protein activator that modulates signaling pathways in roots, resulting in root growth arrest. This compound has been shown to decrease root cell viability in the Col-0 accession. Notably, DFPM exhibits light sensitivity in aqueous solutions and becomes bioactive through light and oxygen-dependent modifications, making it a valuable tool for studying plant defense mechanisms and root development processes.

AFM-30a is a selective inhibitor of protein arginine deiminase 2 (PAD2), exhibiting an EC50 of 9.5 μM for PAD2 binding. This compound effectively inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a is useful for investigating the role of PAD2 in various biological processes, particularly in cancer research and the study of autoimmune diseases such as rheumatoid arthritis, multiple sclerosis, lupus, and ulcerative colitis.

AFM32a is a selective inhibitor of protein arginine deiminase 2 (PAD2), characterized by its benzimidazole structure. This compound demonstrates a remarkable selectivity, exhibiting a 95-fold preference for PAD2 over PAD4 and a 79-fold preference over PAD3. Its potential applications in biochemical research include investigations into the role of PAD2 in various physiological and pathological processes, making it a valuable tool for studying citrullination and related signaling pathways.

PAD4-IN-2 is a selective inhibitor of the peptidyl arginine deiminase 4 (PAD4) enzyme, with an IC50 value of 1.94 μM. This compound has been shown to inhibit tumor growth in mouse models by specifically targeting the PAD4-H3cit-neutrophil extracellular traps (NETs) pathway in neutrophils. PAD4-IN-2 is useful for research applications exploring cancer biology, inflammation, and neutrophil function.

TDFA is an irreversible inhibitor of protein arginine deiminase 4 (PAD4), a crucial enzyme involved in the modification of arginine residues to citrulline. This compound exhibits significant biological activity by affecting histone modifications and autoimmunity-related processes. TDFA is valuable for research applications focusing on rheumatoid arthritis, cancer biology, and neurodegenerative diseases, providing insights into the role of PAD4 in various disease mechanisms.

(Rac)-Cl-amidine is a potent inhibitor of protein arginine deiminase (PAD), demonstrating oral bioavailability and effective inhibition of PAD activity. This compound serves as a valuable tool for investigating PAD functions in cellular contexts, influencing critical biological processes such as gene transcription, cell differentiation, and innate immune responses. Its ability to stabilize epigenetic modifications makes (Rac)-Cl-amidine an important reagent for research in immunology and epigenetics.

2-PADQZ is a potent inhibitor targeting Protein Arginine Deiminase, demonstrating significant antiviral activity against influenza viruses. It specifically binds to the RNA promoter of the influenza A virus, creating a binding site within the internal loop, which disrupts viral replication. Research involving 2-PADQZ has shown notable inhibitory effects against H1N1, H3N2, and influenza B viruses, making it a valuable tool for investigations into antiviral therapeutics and influenza virus biology.

PAD4-IN-5 is a potent inhibitor of the enzyme PAD4, exhibiting an IC50 of ≤10 nM under 50 µM Ca2+ conditions and between 101-500 nM under 1 mM Ca2+ conditions. This compound serves as a valuable tool for investigating the role of PAD4 in autoimmune diseases, particularly rheumatoid arthritis. Its specificity and efficacy make it suitable for research focused on the pathophysiology of these disorders and the development of targeted therapies.

F-Amidine TFA is a selective inhibitor of Protein Arginine Deiminase 4 (PAD4), an enzyme crucial in the process of citrullination, which impacts various inflammatory and autoimmune conditions. This compound has demonstrated significant potential in the study of diseases such as rheumatoid arthritis by modulating PAD4 activity. F-Amidine TFA serves as a valuable tool for researchers exploring the role of PAD4 in immune system dysregulation and related pathologies.

PAD3-IN-1 is a selective inhibitor of protein arginine deiminase 3 (PAD3), exhibiting over 10-fold selectivity compared to PAD isoforms 1, 2, and 4. With IC50 values of 120 μM for PAD1, 27.5 μM for PAD2, 4.5 μM for PAD3, and 30.5 μM for PAD4, PAD3-IN-1 is particularly effective for targeting PAD3. This isoform is implicated in neurodegenerative processes following spinal cord injury, allowing PAD3-IN-1 to serve as a valuable tool for investigating PAD-related neurological disorders.

GSK147 is a potent inhibitor of Peptidylarginine Deiminase 4 (PAD4), demonstrating a Kd of 0.47 µM. This compound effectively inhibits ionomycin-induced protein citrullination in isolated human neutrophils, making it a valuable tool for studying PAD4 activity and its role in various inflammatory conditions. GSK147 is applicable in research focusing on autoimmune diseases and the modulation of protein citrullination.

PAD4-IN-3 is a potent inhibitor of protein arginine deiminase 4 (PAD4), exhibiting notable antitumor activity both in vitro and in vivo. It is designed to be covalently linked to an RGD sequence peptide-modified chitosan, resulting in an oxidative stress-responsive nanoagent. This composite, K-CRGDV-PAD4-IN-3, targets tumors effectively, inhibits PAD4 activity, and suppresses the formation of neutrophil extracellular traps (NETs), thereby enhancing the tumor immune microenvironment. Its applications in cancer research focus on improving therapeutic responses and understanding immune modulation within the tumor context.

BB-Cl-Yne is a selective inhibitor of protein arginine deiminases (PADs), demonstrating Ki values of 6400, 3600, 10800, and 4900 M-1min-1 for PAD1 to PAD4, respectively. This compound serves as a valuable tool for studying PAD enzymatic activity and its role in various biological processes. Additionally, BB-Cl-Yne can be utilized as a click probe for labeling PAD, facilitating research in epigenetics and signal transduction.

BB-F-Yne is a potent inhibitor of protein arginine deiminases (PADs), exhibiting Ki values of 2050, 1700, 1100, and 3100 M^-1 min^-1 for PAD1 through PAD4, respectively. This compound serves as an effective click probe for labeling PAD, facilitating research into its biological roles. BB-F-Yne is valuable for studies investigating the modulation of PAD activity and its implications in various physiological and pathological processes.

F-Amidine is an inhibitor of Protein arginine deiminase 4 (PAD4), a key enzyme involved in the regulation of protein citrullination. This compound is valuable for studying its role in inflammatory and immune system disorders, particularly in conditions such as rheumatoid arthritis. Researchers can utilize F-Amidine to explore the molecular mechanisms underlying immune responses and identify potential therapeutic targets for related diseases.

GSK199 analog hydrochloride is a potent inhibitor of protein arginine deiminase 4 (PAD4), an enzyme involved in the post-translational modification of arginine residues. This compound exhibits promising anti-inflammatory properties and is being explored for therapeutic applications in various autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus, and vasculitis. Additionally, it shows potential in the treatment of oncological conditions and other disorders characterized by dysregulated citrullination, making it a valuable tool for researchers investigating these diseases.

Citrulline-specific probe-biotin is a biotinylated fluorescent probe designed for the detection of citrulline, a hydrolysis product of arginine produced by the enzyme protein arginine deiminase (PAD). Increased PAD activity is implicated in various pathological conditions, including autoimmune diseases and inflammatory disorders. This probe facilitates the identification of diseases characterized by elevated citrulline levels and is particularly useful in animal models of ulcerative colitis for studying disease mechanisms and potential therapeutic interventions.