| Name | Devimistat |
| Description | Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others. |
| In vitro | In vitro, Devimistat produces the selective toxicity against several tumor cell lines including H460 human lung cancer cells and Saos-2 human sarcoma cells with EC50 of 120 μM and 120 μM, respectively. Devimistat disrupts H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity and loss of mitochondrial membrane potential in a time- and drug dose-dependent fashion. In addition, Devimistat (240 μM) also induces both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells. [1] |
| In vivo | Devimistat (25 mg/kg) has potent anticancer activity in a human tumor xenograft model of of a pancreatic tumor cell (BxPC-3). Similarly, Devimistat (10 mg/kg) also produces significant tumor growth inhibition of H460 human non-small cell lung carcinoma in mouse model. Besides, Devimistat produces little or no side-effect toxicity in expected therapeutic dose ranges in large animal models and has the maximum tolerated dose of 100 mg/kg in mice. [1] |
| Storage | Store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 78 mg/mL (200.73 mM), Sonication is recommended.
DMSO : 250 mg/mL (643.35 mM), Sonication is recommended.
10% DMSO+90% Corn oil : 10 mg/mL (25.73 mM), Solution.
10% DMSO+90% (20% SBE-β-CD in Saline) : < 10 mg/mL (25.73 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% Saline : < 10 mg/mL (25.73 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 10 mg/mL (25.73 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
H2O : < 1 mg/mL (insoluble or slightly soluble)
|
| Keywords | α-ketoglutarate dehydrogenase | PDH | MitochondrialMetabolism | Mitochondrial Metabolism | mitochondrial | ipoic | Inhibitor | inhibit | Devimistat | cancer | Apoptosis | acid | abrogates |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Imeglimin hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Reprogramming Compound Library | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
