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MA242
CAS No. : 1049704-18-8
MCE 国际站：MA242
产品活性：MA242 是特异性的 MDM2 和 NFAT1 双重抑制剂。MA242 以高亲和力直接结合 MDM2 和 NFAT1，诱导 MDM2 和 NFAT1 蛋白降解，并抑制 NFAT1 介导的 MDM2 转录。MA242 在胰腺癌细胞系中诱导凋亡。
研究领域：Apoptosis
In Vitro: MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells.
MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines.
MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity.
MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM.
In Vivo: MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53.
There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses.
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文献和实验.Chromatogr.A,1997,790:11～19［12］Berger T A.J.Chromatogr.A,1997,785:3～33［13］Yeh C S,Yu T,Berthod Alain.J.Liq.Chrom.& Rel.Technol.,1999,22(3):345～356［14］Tsai Y-L,Yu T.J.Chromatogr.A,1999,835(1-2):237～242［15］Abbott T P,Kleiman R.J.Chromatogr.,1991,538:109～118［16］
0.lμg。器材和试剂1.器材(1)电泳仪、琼指糖电泳槽。(2)20μl微量加液器。(3)透射式紫外分析仪。2.试剂(1)50X TAETris—HCl 242. 2g与冰乙酸57.1ml加水至1000ml0.5M EDTA(pH8.0)100ml(2)载样指示液25mg溴酚兰溶解于100ml40%蔗糠中。(3)1%溴化乙锭。 (4)电泳液： 1000ml lX TAE 加90ml 1%溴化乙锭 1g溴化乙锭加水100ml，充分溶解后，倒入棕色瓶中，避光
Computational Large‐Scale Mapping of Protein‐Protein Interactions Using Structural Complexes
., Weissig, H., Shindyalov, I.N., and Bourne, P.E. 2000. The Protein Data Bank. Nucleic Acids Res 28:235‐242. Camacho, C., Coulouris, G., Avagyan, V., Ma, N., Papadopoulos, J
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