Molecular Formula | C20H24ClN3O4S |
Molar Mass | 437.94 |
Density | 1.327±0.06 g/cm3(Predicted) |
Boling Point | 547.2±45.0 °C(Predicted) |
Physical and Chemical Properties | Acidity coefficient (pKa) 6.12±0.50(Predicted) |
biological activity
Stenabolic (SR9009) is a synthetic REV-ERB agonist. The IC50 values for REV-ERB-α and REV-ERB-β are 670 nM and 800 nM, respectively.
target
Target Value
REV-ERB-α
(HEK293 cells) 670 nM
REV-ERB-β
(HEK293 cells) 800 nM
in vitro study
SR9009 has a lethal effect on cancer cells and aging cells induced by oncogenes (including melanocytic nevus), but has no effect on the vitality of normal cells and tissues. SR9009 regulates autophagy and lipid neogenesis, which plays a key role in inducing apoptosis in malignant cells. The treatment of cancer cells was treated with SR9009. By detecting caspase3 splicing and TUNEL test, the treatment of SR9009 cancer cells reduced their cell viability because apoptosis was induced. SR9009 reduces the number of autophagosomes, thus inhibiting autophagy.
in vivo studies
In food-borne obese mice, SR9909 can cause a decrease in fat mass and blood lipids. In vivo, SR9009 can inhibit the growth of malignant glioma and improve its survival rate in mice without causing obvious toxicity. SR9009 can penetrate the blood-brain barrier and inhibit tumor growth in a transplanted tumor model using malignant glioma migration from patients. In two different malignant glioma models, the survival rate is significantly improved.