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

PAD4-IN-4 Estructura química

No. CAS : 3044006-76-7

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PAD4-IN-4 Related Antibodies

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Descripciòn

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)

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
2.39 μM
Compound: 28
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
MCF-10A IC50
8.39 μM
Compound: 28
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
MDA-MB-468 IC50
2.34 μM
Compound: 28
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
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.
Peso molecular

567.08

Fòrmula

C32H31ClN6O2
No. CAS
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
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Room temperature in continental US; may vary elsewhere.
Almacenamiento

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Referencias
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PAD4-IN-4 Related Classifications

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  • 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-43044006-76-7Protein Arginine DeiminasePeptidylarginine DeiminasePAD4 InhibitorTriple-negative breast cancerTNBC cellsorthotopic 4T1-luc xenograft modelInhibitorinhibitorinhibit

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