WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406486
Description: MPT0E028 is a novel N-hydroxyacrylamide-derived HDAC inhibitor, inhibited human colorectal cancer HCT116 cell growth in vitro and in vivo. The results of NCI-60 screening showed that MPT0E028 inhibited proliferation in both solid and hematological tumor cell lines at micromolar concentrations, and was especially potent in HCT116 cells. MPT0E028 had a stronger apoptotic activity and inhibited HDACs activity more potently than SAHA, the first therapeutic HDAC inhibitor proved by FDA. In vivo murine model, the growth of HCT116 tumor xenograft was delayed and inhibited after treatment with MPT0E028 in a dose-dependent manner. Based on in vivo study, MPT0E028 showed stronger anti-cancer efficacy than SAHA. No significant body weight difference or other adverse effects were observed in both MPT0E028-and SAHA-treated groups. Taken together, our results demonstrate that MPT0E028 has several properties and is potential as a promising anti-cancer therapeutic drug. ( PLoS One. 2012;7(8):e43645.)
MedKoo Cat#: 406486
Chemical Formula: C17H16N2O4S
Exact Mass: 344.08308
Molecular Weight: 344.38494
Elemental Analysis: C, 59.29; H, 4.68; N, 8.13; O, 18.58; S, 9.31
Synonym: MPT-0E028; MPT0E028; MPT 0E028
IUPAC/Chemical Name: (E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide
InChi Key: MGTIFSBCGGAZDB-VQHVLOKHSA-N
InChi Code: InChI=1S/C17H16N2O4S/c20-17(18-21)9-7-13-6-8-16-14(12-13)10-11-19(16)24(22,23)15-4-2-1-3-5-15/h1-9,12,21H,10-11H2,(H,18,20)/b9-7+
SMILES Code: O=C(NO)/C=C/C1=CC2=C(N(S(=O)(C3=CC=CC=C3)=O)CC2)C=C1
MPT0E028 enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells.
1: Chen CH, Chen MC, Wang JC, Tsai AC, Chen CS, Liou JP, Pan SL, Teng CM. Synergistic Interaction between the HDAC Inhibitor, MPT0E028, and Sorafenib in Liver Cancer Cells In Vitro and In Vivo. Clin Cancer Res. 2014 Mar 1;20(5):1274-87. doi: 10.1158/1078-0432.CCR-12-3909. Epub 2014 Feb 11. PubMed PMID: 24520095.
2: Chen MC, Chen CH, Wang JC, Tsai AC, Liou JP, Pan SL, Teng CM. The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells. Cell Death Dis. 2013 Sep 19;4:e810. doi: 10.1038/cddis.2013.330. PubMed PMID: 24052078; PubMed Central PMCID: PMC3789188.
3: Huang HL, Lee HY, Tsai AC, Peng CY, Lai MJ, Wang JC, Pan SL, Teng CM, Liou JP. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. doi: 10.1371/journal.pone.0043645. Epub 2012 Aug 22. Erratum in: PLoS One. 2012;7(9). doi: 10.1371/annotation/ab4fff87-6a32-4718-aa4c-91658f164b8d. Huang, Han-Lin [corrected to Huang, Han-Li]. PubMed PMID: 22928010; PubMed Central PMCID: PMC3425516.