2. Epigenetics
  3. Protein Arginine Deiminase
  4. PAD4-IN-4

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.

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PAD4-IN-4 Chemical Structure

PAD4-IN-4 Chemical Structure

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PAD4-IN-4 Related Antibodies

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Description

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[1].

IC50 & Target[1]

PAD4

0.79 μM (IC50)

PAD2

2.97 μM (IC50)

In Vitro

PAD4-IN-4 displays substantial inhibitory activity toward PAD2 and PAD4 (IC50=2.97 ± 0.29 and 0.79 ± 0.09 μM), with the best PAD4 selectivity[1].
PAD4-IN-4 suppresses the proliferation of TNBC cells in vitro (4T1 IC50: 2.39 ± 0.54 μM; MDA-MB468 IC50: 2.34 ± 0.23 μM), with relatively low toxicity toward normal breast cells (MCF-10A IC50: 8.39 ± 0.60 μM)[1].
PAD4-IN-4 (0.5, 1, 2 μM; 48 h) has enhanced antimetastasis activity for TNBC cells[1].
PAD4-IN-4 (0.5, 1, 2 μM; 48 h) is a potent PAD4 inhibitor for blocking histone citrullination and neutrophil extracellular trap (NET) formation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PAD4-IN-4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: TNBC cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Reduced the number of metastatic cells and wound closure rate less than that of 7 at the equivalent dose, indicating that compound 28 had enhanced antimetastasis activity.

Immunofluorescence[1]

Cell Line: TNBC cells and neutrophils
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Inhibited histone citrullination and NET formation.
In Vivo

PAD4-IN-4 (1, 5, 10 mg/kg; i.v.; every 2 days for a total of nine times) can dosedependently suppress the lung metastasis of TNBC. PAD4-IN-4 is a promising candidate against TNBC without obvious toxicity in orthotopic 4T1-luc xenograft model in BALB/c mice[1].
PAD4-IN-4 alters the tumor microenvironment from a suppressive condition to an antitumor milieu by modulating the proportion of immune cells and reshaping the neutrophil phenotype and function[1].
Pharmacokinetic Analysis in Male Sprague−Dawley rats[1]

Compound Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L•h/kg)
7 i.v. 3.5 14893.52 17214.17 0.13 0.08 251.2 571.87
28 i.v. 3.5 9525.86 17346.55 0.25 0.08 297.71 105.24

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: orthotopic 4T1-luc xenograft model in BALB/c mice[1].
Dosage: 1, 5, 10 mg/kg
Administration: Intravenous injection (i.v.)
Result: The tumor growth inhibition of the high-dose 28-treated group was 61.8%, whereas the positive control doxorubicin hydrochloride group reached 54.6%.
Had no significant differences in viscero−somatic ratio and serum biochemical indices (ALT, AST, UREA, and CREA-S) were observed in the 28-treated group.
Increased the proportion of mature TANs MHC-II+ TANs whereas it suppressed the proportion of pro-tumor phenotypes PD-L1+ /MHC-II+ TANs and MHC-II− TANs.
Molecular Weight

567.08

Formula

C32H31ClN6O2
SMILES

O=C(C1=CC2=C(C(C3=CC=CC=C3)=N1)NC4=C2C=CC=C4)N[C@H](C(NCC5=CC=CC=C5)=O)CCCNC(CCl)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PAD4-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PAD4-IN-4Protein Arginine DeiminasePeptidylarginine DeiminasePAD4 InhibitorTriple-negative breast cancerTNBC cellsorthotopic 4T1-luc xenograft modelInhibitorinhibitorinhibit

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