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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
38 Results for "
PAD4
" in MedChemExpress (MCE) Product Catalog:
Products (38)
38 Results for "PAD4" in MCE Product Catalog:
54
54 Publications Verification
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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.
54
54 Publications Verification
Cat. No.: HY-123606
CAS No.: 1652629-23-6
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GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8 + T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions [4] .
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24 Cited Publications
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Cl-amidine hydrochloride 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 hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model [4] .
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24 Cited Publications
Cat. No.: HY-100574B
CAS No.: 1043444-18-3
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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. 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 [4] .
2
2 Cited Publications
Synonyms: PAD2-IN-1 hydrochloride
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AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .
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2 Cited Publications
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GSK199 is an orally active, reversible, and selective PAD4 inhibitor with an IC50 of 200 nM in the absence of calcium. GSK199 can be used for the research of rheumatoid arthritis .
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1
1 Cited Publications
Cat. No.: HY-P70990
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: PADI4; Protein-Arginine Deiminase Type IV; Prev. PADI5; HL-60 PAD; PDI5; PAD4; PDI4; Peptidyl Arginine Deiminase Type IV; PAD; Peptidylarginine Deiminase IV; Peptidyl Arginine Deiminase, Type IV; PADI-H Protein; Peptidyl Arginine Deiminase, Type V; PADI4
Cat. No.: HY-176710
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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 Ca 2+-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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JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
Cat. No.: HY-100574
CAS No.: 913723-61-2
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Cl-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 [4] .
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BMS-P5 is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
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BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model .
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PAD-IN-2 is a potent pad4 inhibitor (IC50: <1 μM). PAD-IN-2 can be used in the research of auto-immune diseases and cancers, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis and psoriasis .
Cat. No.: HY-155052
CAS No.: 2642327-52-2
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PAD4-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 .
Cat. No.: HY-155052A
Purity: 95.64%
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PAD4-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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GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199 .
Cat. No.: HY-136557
CAS No.: 2095109-82-1
Synonyms: PAD2-IN-1
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AFM32a (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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GSK121 is a selective PAD4 inhibitor. GSK121 can be used in the research of PAD4-related diseases, including those characterized by abnormal NET levels and various tumors .
Cat. No.: HY-P1417
CAS No.: 1345019-64-8
Synonyms: Thr-Asp-F-amidine
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
