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Cardiovascular Disease Inflammation/Immunology Cancer

Research Areas:

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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61

GSK484

61 Publications Verification

Cat. No.: HY-123606

CAS No.: 1652629-23-6

Target:

Protein Arginine Deiminase MHC

Research Areas:

Cardiovascular Disease Inflammation/Immunology

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 .

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28

Cl-amidine hydrochloride

28 Cited Publications

Cat. No.: HY-100574A

CAS No.: 1373232-26-8

Purity: 99.82%

Target:

Protein Arginine Deiminase Apoptosis MicroRNA

Research Areas:

Protein Arginine Deiminase Apoptosis MicroRNA

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 .

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28

Cl-amidine TFA

28 Cited Publications

Cat. No.: HY-100574B

CAS No.: 1043444-18-3

Target:

Research Areas:

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 .

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17

Eeyarestatin I

17 Cited Publications

Cat. No.: HY-110078

CAS No.: 412960-54-4

Purity: 99.56%

Target:

p97 Apoptosis

Research Areas:

Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects .

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12

BB-Cl-Amidine

12 Cited Publications

Cat. No.: HY-111347

CAS No.: 1802637-39-3

Purity: 95.65%

Target:

Research Areas:

Inflammation/Immunology

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

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12

BB-Cl-Amidine hydrochloride

12 Cited Publications

Cat. No.: HY-111347A

CAS No.: 2436747-41-8

Purity: 99.47%

Target:

Research Areas:

Inflammation/Immunology

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

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3

AFM32a hydrochloride

3 Cited Publications

Cat. No.: HY-136557A

CAS No.: 2988594-85-8

Purity: 99.71%

Synonyms: PAD2-IN-1 hydrochloride

Target:

Research Areas:

Pyridine Alkaloids Infection Alkaloids Quinones Microorganisms Monophenols Phenols Benzene Quinones Disease Research Fields Cancer

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

Streptonigrin

2 Cited Publications

Cat. No.: HY-124586

CAS No.: 3930-19-6

Purity: 99.20%

Synonyms: Bruneomycin

Category:

Target:

Antibiotic Protein Arginine Deiminase E1/E2/E3 Enzyme HIF/HIF Prolyl-Hydroxylase MDM-2/p53 Apoptosis

Streptonigrin (Bruneomycin) is an orally active antibiotic and pan-PAD inhibitor, inhibiting PAD1, PAD2, PAD3 and PAD4 with IC₅₀ of 48.3 μM, 26.1 μM, 0.43 μM and 2.5 μM, respectively. Streptonigrin inhibits SENP1 (IC₅₀ of 0.518 μM) and reduces HIF1α. Streptonigrin increases p53 and Apoptosis. Streptonigrin shows antiviral activity against Rauscher murine leukemia virus. Streptonigrin has immunosuppressive effects. Streptonigrin has antitumor activity against osteosarcoma .

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2

GSK199

2 Cited Publications

Cat. No.: HY-103058

CAS No.: 1549811-53-1

Purity: 99.85%

Target:

Cardiovascular Disease Inflammation/Immunology Cancer

Research Areas:

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

AFM-30a hydrochloride

1 Cited Publications

Cat. No.: HY-125099A

Purity: 99.83%

Target:

Research Areas:

Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Cancer

AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC₅₀ value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC₅₀ value of 0.4 μM. AFM-30a hydrochloride 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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1

Acefylline

1 Cited Publications

Cat. No.: HY-B1505

CAS No.: 652-37-9

Synonyms: Theophyllineacetic acid; Theophylline-7-acetic acid

Category:

Target:

Adenosine Receptor Protein Arginine Deiminase Phosphodiesterase (PDE)

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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1

PADI4 Protein, Human (His)

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

Species:

Human

Source:

E. coli

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PAD-PF2

Cat. No.: HY-176710

Target:

Protein Arginine Deiminase Opioid Receptor mAChR

Research Areas:

Neurological Disease Inflammation/Immunology Cancer

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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Cl-amidine

Cat. No.: HY-100574

CAS No.: 913723-61-2

Target:

Protein Arginine Deiminase Apoptosis MicroRNA

Research Areas:

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 .

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JBI-589

Cat. No.: HY-153450

CAS No.: 2308504-22-3

Purity: 99.75%

Target:

Research Areas:

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 .

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PAD-IN-2

Cat. No.: HY-135304

CAS No.: 2304852-21-7

Purity: 99.29%

Target:

Research Areas:

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 .

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BMS-P5

Cat. No.: HY-137655

CAS No.: 1549811-36-0

Purity: 99.23%

Target:

Research Areas:

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

Cat. No.: HY-137655A

CAS No.: 1550371-22-6

Purity: 99.93%

Target:

Research Areas: