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Class I and II histone deacetylase (HDAC) inhibitor (IC50 = 0.045 μM; EC50 = 0.025 μM in HeLa screening and HeLa cell-based assays, respectively). Exhibits broad spectrum inhibition of HDAC classes I and II in assays using purified recombinant human isoforms. Displays less potent inhibition of HDAC2 (IC50 values are 0.014, 0.020, 0.026, 0.075 and 2.0 μM for HDAC6, HDAC1, HDAC4, HDAC3 and HDAC2 respectively). Displays cytotoxicity against numerous cell lines derived from human tumors. Orally available.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Feng et al (2008) KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling. Mol.Cancer Ther. 7 1494 PMID: 18566220
Hassig et al (2008) KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad-spectrum antitumor activity in vitro and in vivo. Mol.Cancer Ther. 7 1054 PMID: 18483295
Payne et al (2008) Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor. Bioorg.Med.Chem.Lett. 18 6093 PMID: 18954983
Keywords: KD 5170, KD 5170 supplier, antitumor, antitumour, hdacs, histone, deacetylases, inhibitors, inhibits, KD5170, epigenetics, Non-selective, HDACs, Non-Selective, 4001, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.