MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity.
MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS).
MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program.
性状
Solid
体外研究(In Vitro)
MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells.
MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression.
MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR
Cell Line:
MDA-MB-231 cells
Concentration:
6 μM; 8 μM
Incubation Time:
24 hours
Result:
Increased MMP13 mRNA expression.
Western Blot Analysis
Cell Line:
HeLa cells
Concentration:
2 μM; 4 μM; 6 μM; 8 μM; 10 μM
Incubation Time:
24 hours
Result:
Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression.
Cell Viability Assay
Cell Line:
SRC-3 KO and WT HeLa cells
Concentration:
3 μM; 4 μM; 5 μM; 6 μM; 7 μM
Incubation Time:
24 hours
Result:
Decreased SRC-3 KO and WT HeLa cell viability.
体内研究(In Vivo)
MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)