MCB-613-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMCB-613Cat. No.: HY-19625CAS No.: 1162656-22-5分式: CHNO分量: 304.39作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (164.26 mM; Need ultrasonic)H2O : 40% PEG300 5

2、% Tween-80 45% salineSolubility: 2.5 mg/mL (8.21 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.21 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (8.21 mM); Clear solutionBIOLO

3、GICAL ACTIVITY物活性 MCB-613種有效的類 醇受體共激活因 (SRC) 分“刺激物” (SMS)，超刺激 SRCs 的轉(zhuǎn)錄活性。MCB-613 增加了 SRC 與其他共激活因的相互作，并顯 誘導 ER 應激與活性氧 (ROS) 的產(chǎn)相結(jié)合。MCB-613 種 SMS，通過過度刺激 SRC 致癌程序，靶向癌 因作抗癌藥物。體外研究 MCB-613 (6-8 M; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells1.MCB-613 (2-10 M; 4 hours) leads to

4、proteasome dysfunction and ER stress, the induction of the markersfor unfolded protein response (UPR), including the phosphorylation of eIF2 and IRE1 as well as theinduction of ATF4 protein expression 1.MCB-613 (0-7 M; 4 hours) affects SRC-3 KO and WT HeLa cellviability, SRC-3 WT HeLa cell is more a

5、ffected by MCB-613 compared with KO cells 1.RT-PCR 1Cell Line: MDA-MB-231 cellsConcentration: 6 M; 8 MIncubation Time: 24 hoursResult: Increased MMP13 mRNA expression.Western Blot Analysis 1Cell Line: HeLa cellsConcentration: 2 M; 4 M; 6 M; 8 M; 10 MIncubation Time: 24 hoursResult: Induced the p-eIF

6、2, p-IRE1, and ATF-4 protein expression.Cell Viability Assay 1Cell Line: SRC-3 KO and WT HeLa cellsConcentration: 3 M; 4 M; 5 M; 6 M; 7 MIncubation Time: 24 hoursResult: Decreased SRC-3 KO and WT HeLa cell viability.體內(nèi)研究MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly a

7、nd dramatically stalls thegrowth of the tumor compared with the control group and causes no obvious animal toxicity 12/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Model: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7cells into mammary fat pads) 1Dosage: 20

8、mg/kgAdministration: Intravenous injection; 20 mg/kg; 3 times/week; 7 weeksResult: Inhibited tumor growth in vivo.REFERENCES1. Wang L, et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells andLeads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.McePdfHeightCaution: Product has not been fully validated for medical application