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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- CAS No.: 3044006-76-7
- Formule: C32H31ClN6O2
- Masse moléculaire:567.08
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Activité biologique
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Activité biologique
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PAD4 0.79 μM (IC50) |
PAD2 2.97 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
2.39 μM
Compound: 28
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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
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[PMID: 38728549] |
| MCF-10A | IC50 |
8.39 μM
Compound: 28
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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
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[PMID: 38728549] |
| MDA-MB-468 | IC50 |
2.34 μM
Compound: 28
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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
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[PMID: 38728549] |
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.
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Cell Line:TNBC cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:48 h
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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.
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Cell Line:TNBC cells and neutrophils
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Concentration:0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Inhibited histone citrullination and NET formation.
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 |