WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406119
Description: MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.
MedKoo Cat#: 406119
Chemical Formula: C31H30N2O12S3
Exact Mass: 718.09609
Molecular Weight: 718.77
Elemental Analysis: C, 51.80; H, 4.21; N, 3.90; O, 26.71; S, 13.38
Synonym: MT477; MT 477; MT-477
IUPAC/Chemical Name: tetramethyl 6'-(2-(2,5-dioxopyrrolidin-1-yl)acetyl)-7'-methoxy-5',5'-dimethyl-5',6'-dihydrospiro[[1,3]dithiole-2,1'-thiopyrano[2,3-c]quinoline]-2',3',4,5-tetracarboxylate
SMILES Code: O=C(C1=C(C(OC)=O)SC2=C(C31SC(C(OC)=O)=C(C(OC)=O)S3)C4=C(N(C(CN5C(CCC5=O)=O)=O)C2(C)C)C(OC)=CC=C4)OC
1: Ouelaa-Benslama R, De Wever O, Hendrix A, Sabbah M, Lambein K, Land D, PrÃ©vost G, Bracke M, Hung MC, Larsen AK, Emami S, Gespach C. Identification of a GαGβγ, AKT and PKCα signalome associated with invasive growth in two genetic models of human breast cancer cell epithelial-to-mesenchymal transition. Int J Oncol. 2012 Jul;41(1):189-200. doi: 10.3892/ijo.2012.1457. Epub 2012 Apr 30. PubMed PMID: 22552300.
2: Jasinski P, Zwolak P, Terai K, Vogel RI, Borja-Cacho D, Dudek AZ. MT477 acts in tumor cells as an AURKA inhibitor and strongly induces NRF-2 signaling. Anticancer Res. 2011 Apr;31(4):1181-7. PubMed PMID: 21508363.
3: Jasinski P, Zwolak P, Terai K, Borja-Cacho D, Dudek AZ. PKC-alpha inhibitor MT477 slows tumor growth with minimal toxicity in in vivo model of non-Ras-mutated cancer via induction of apoptosis. Invest New Drugs. 2011 Feb;29(1):33-40. doi: 10.1007/s10637-009-9330-9. Epub 2009 Oct 1. PubMed PMID: 19795097.
4: Jasinski P, Zwolak P, Terai K, Dudek AZ. Novel Ras pathway inhibitor induces apoptosis and growth inhibition of K-ras-mutated cancer cells in vitro and in vivo. Transl Res. 2008 Nov;152(5):203-12. doi: 10.1016/j.trsl.2008.09.001. Epub 2008 Oct 11. PubMed PMID: 19010291.
5: Jasinski P, Welsh B, Galvez J, Land D, Zwolak P, Ghandi L, Terai K, Dudek AZ. A novel quinoline, MT477: suppresses cell signaling through Ras molecular pathway, inhibits PKC activity, and demonstrates in vivo anti-tumor activity against human carcinoma cell lines. Invest New Drugs. 2008 Jun;26(3):223-32. Epub 2007 Oct 24. PubMed PMID: 17957339.