Protein Arginine Deiminase Inhibitor

Protein Arginine Deiminase Inhibitors (31):

Cat. No.	Product Name	Effect	Purity

HY-100514

GSK484 hydrochloride	Inhibitor	99.72%
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.

HY-100574A

Cl-amidine hydrochloride	Inhibitor	99.39%
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.

HY-111347A

BB-Cl-Amidine hydrochloride	Inhibitor	99.47%
BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor.

HY-125099A

AFM-30a hydrochloride	Inhibitor	99.96%
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.

HY-136557A

AFM32a hydrochloride	Inhibitor	99.71%
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).

HY-155052A

PAD4-IN-2 TFA	Inhibitor
PAD4-IN-2 (compound 5i) TFA is a PAD4 inhibitor (IC₅₀=1.94 μM). PAD4-IN-2 TFA inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils.

HY-162494

PAD4-IN-4	Inhibitor
PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC₅₀=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research.

HY-137125

BB-Cl-Yne	Inhibitor
BB-Cl-Yne is a protein arginine deiminase (PAD) inhibitor with K_i 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.

HY-103058

GSK199	Inhibitor	99.86%
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.

HY-100574D

D-Cl-amidine hydrochloride	Inhibitor	99.91%
D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.

HY-137655A

BMS-P5 free base	Inhibitor	99.96%
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.

HY-135304

PAD-IN-2	Inhibitor	99.02%
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.

HY-117777

GSK121	Inhibitor	99.81%
GSK-121 Trifluoroacetates a selective PAD4 inhibitor.

HY-124586

Streptonigrin	Inhibitor	99.20%
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 µM, 26.1±0.3 µM, 0.43±0.03 µM, and 2.5±0.4 µM for PAD1, PAD2, PAD3, and PAD4, respectively.

HY-153450

JBI-589	Inhibitor	98.93%
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.

HY-120343

GSK106	Inhibitor	98.00%
GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199.

HY-111347

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

HY-125099

AFM-30a	Inhibitor
AFM-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.

HY-136557

AFM32a	Inhibitor
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).

HY-100574

Cl-amidine	Inhibitor
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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