| Field | Specification |
|---|---|
| Applications | |
| Molecular weight | |
| Molecular formula | C20H21N3O5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Neutrophil elastase inhibitor 4 is an inhibitor of human neutrophil elastase (HNE), with an IC50 of 21.78 nM and a Ki of 8.04 nM. It induces G2/M cell cycle arrest and apoptosis, and is applicable to research on breast cancer, multiple myeloma and non-small cell lung cancer[1]. It has a molecular formula of C20H21N3O5 and a molecular weight of 383.40 g/mol.
Physical & Chemical Properties
| Molecular Formula | C20H21N3O5 |
|---|---|
| Molecular Weight | 383.40 g/mol |
| SMILES | O=C(C(N(CC1=C2C=CC=C1N3C(C(CC)(CC)C3=O)=O)C2=O)CC4)NC4=O |
| Signaling Pathway | Metabolic Enzyme/Protease; Apoptosis |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
42.30 nM human neutrophil elastase[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In T47D, RPMI 8226 and A549 cancer cells, Neutrophil elastase inhibitor 4 (72 h) potently inhibits proliferation, with IC50 values of 21.25, 34.17 and 29.93 μM, and it shows high selectivity toward normal human skin fibroblasts[1]. In T47D breast cancer cells, Neutrophil elastase inhibitor 4 (5-40 μM; 48 h) triggers apoptotic cell death in a concentration-dependent manner and induces G2/M cell cycle arrest[1].
Apoptosis Analysis[1]
| Cell Line | human T47D breast carcinoma cells |
|---|---|
| Concentration | 5, 10, 20, and 40 μM |
| Incubation Time | 48 h |
| Result | Induced concentration-dependent apoptosis: the percentage of apoptotic cells increased from 2.17% (control) to 3.99%, 13.99%, 21.54%, and 34.49% at 5, 10, 20, and 40 μM, respectively. Necrosis also increased at 20 and 40 μM (to 10.52% and 9.77%, respectively, from 2.19% control). Was over four times more potent at inducing apoptosis than lenalidomide at 20 μM. |
Cell Cycle Analysis[1]
| Cell Line | human T47D breast carcinoma cells |
|---|---|
| Concentration | 5, 10, 20, and 40 μM |
| Incubation Time | 48 h |
| Result | Induced concentration-dependent G2/M phase arrest: at 5, 10, 20, and 40 μM, the percentage of cells in G2 phase increased from 15.77% (control) to 17.83%, 24.68%, 26.11%, and 22.82%, respectively, while G1 phase cell numbers decreased. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Panton-Valentine leukocidin-induced neutrophil extracellular traps lack antimicrobial activity and are readily induced in patients with recurrent PVL+-Staphylococcus aureus infections. J Leukoc Biol 2024 Jan 19;115(2):222-234. PMID: 37943843
