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6,8-Bis(benzylthio)octanoic acid is a pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase (KGDH) inhibitor. Disrupts tumor cell mitochondrial metabolism, and increases mitochondrial reactive oxygen species (ROS) production in H460 lung carcinoma cells. Has no effect on KGDH activity in normal bronchial epithelial cells. Induces cell death of multiple tumor cell lines selectively over normal cells in vitro. Inhibits tumor growth of H460 and BxPC-3 tumor cell xenografts in mice.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 388.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.57 mL||12.87 mL||25.73 mL|
|5 mM||0.51 mL||2.57 mL||5.15 mL|
|10 mM||0.26 mL||1.29 mL||2.57 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the biological activity of the product.
Zachar et al (2011) Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo. J.Mol.Med. (Berl.) 89 1137 PMID: 21769686
Stuart et al (2014) A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process. Cancer Metab. 2 4 PMID: 24612826
Egawa et al (2018) Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma. PLoS One 13 e0198940 PMID: 29879220
If you know of a relevant reference for 6,8-Bis(benzylthio)octanoic acid, please let us know.
Keywords: 6,8-Bis(benzylthio)octanoic acid, 6,8-Bis(benzylthio)octanoic acid supplier, 6,8-Bis(benzylthio)octanoic, acid, CPI613, Pyruvate, dehydrogenase, PDH, a-ketoglutarate, alpha, KGDH, inhibitors, inhibits, antitumor, active, in, vivo, xenografts, cell, death, Other, Dehydrogenases, 5348, Tocris Bioscience
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