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HA14-1 is a small molecule which has the potential of inducing apoptosis in cancerous cells. HA14-1 manifests an antagonistic effect on antiapoptotic protein Bcl-2 and consequently induces cell death in various cancerous cell lines. HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.P53 pathway to be the probable mechanism of action for the induction of apoptosis in HeLa cell by downregulating the effect of anti-apoptotic proteins suggesting that HA14-1 may provide therapeutic potential for the treatment of human cervical cancer.
| Cell Experiment | |
|---|---|
| Cell lines | HF1A3, HF4.9 and HF28RA cells |
| Preparation method | Determining the cytotoxic effects of HA14-1 against different FL cell lines by the MTT assay. Briefly, incubating the cells (5000/well) in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, adding the MTT solution to each well. After 4 h incubation at 37 °C, measuring the optical density (OD) by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) ?100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw |
| Concentrations | ~25 μM |
| Incubation time | 20 h |
| Animal Experiment | |
|---|---|
| Animal models | Female Swiss nude mice bearing BeGBM xenografts |
| Formulation | Free RPMI 1640-50% DMSO. |
| Dosages | 400 nM |
| Administration | Inject at the site of cell injection. |
| Molecular Weight | 409.23 |
| Formula | C17H17BrN2O5 |
| CAS Number | 65673-63-4 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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