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In vitro: SM-164 induced complete cIAP-1 degradation, it displayed weak inhibitory effects on the viability of HCC cells. Nevertheless, SM-164 considerably potentiated Apo2 ligand or TNF-related apoptosis-inducing ligand (APO2L/TRAIL)- and Doxorubicin-mediated anticancer activity in HCC cells. Mechanistic studies demonstrated that SM-164 in combination with chemotherapeutic agents resulted in enhanced activation of caspases-9, -3 and cleavage of poly ADP-ribose polymerase (PARP), and also led to decreased AKT activation. Although SM-164 is modestly more effective than SM-122 in induction of cIAP-1/2 degradation, SM-164 is 1,000 times more potent than SM-122 as an inducer of apoptosis in tumor cells, which is attributed to its much higher potency in binding to and antagonizing XIAP. SM-164 radiosensitization in sensitive cells was associated with NF-κB activation and TNFα secretion, followed by activation of caspase-8 and -9, leading to enhanced apoptosis.
In vivo: SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. SM-164 also radiosensitized human tumor xenograft while causing minimal toxicity.
| Cell Experiment | |
|---|---|
| Cell lines | Breast cancer lines, including SK-BR-3, MDA-MB-468, MDA-MB-453, MCF-7, ZR-75-1, T-47D |
| Preparation method | Cell were seeded in 96-well plates in triplicate and treated the next day with SM-164 in various doses ranging from 0.03 to 10 μM for 24 h. The viability of the cells was then measured using one-step ATPlite cell proliferation assay. |
| Concentrations | 0.03 to 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 1121.42 |
| Formula | C62H84N14O6 |
| CAS Number | 957135-43-2 |
| Solubility (25°C) | 10 mM in 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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| LBW242
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