MCB-613

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MCB-613 是一种有效的类固醇受体共激活剂 (SRC) 刺激剂。

MCB-613 is a potent Steroid Receptor Coactivator Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. MCB-613 can super-stimulate 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 selectively induce excessive stress in cancer cells. Over-stimulating the SRC oncogenic program can be an effective strategy to kill cancer cells. By integrating growth pathways on which cancer cells rely, steroid receptor coactivators (SRC-1, SRC-2, and SRC-3) represent emerging targets in cancer therapeutics.

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.RT-PCRCell 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.

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 Animal Model:MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)Dosage:20 mg/kg Administration:Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks Result:Inhibited tumor growth in vivo.

MCB-613 | MCB 613 | MCB613

Immunology/Inflammation

Hydroxylase

Src

Cancer

——

1162656-22-5

304.39

C20H20N2O

>98% (HPLC)

DMSO : 50 mg/mL 164.26 mM; H2O : < 0.1 mg/mL

C1(C/C(=C\c2cnccc2)/C(=O)/C(=C/c2cnccc2)/C1)CC

(3E,5E)-1-ethyl-3,5-bis(pyridin-3-ylmethylene)piperidin-4-one

(-20℃)

With Ice Pack

≥ 2 years