| Name | TEPP-46 |
| Description | TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity. |
| In vitro | METHODS: Human hepatocellular carcinoma cells, HepG2, were treated with TCEP hydrochloride (100-400 µM) for 3 days, and cell viability was measured by MTT assay.
RESULTS: The viability of HepG2 was significantly reduced to 25.68% and 70.92% after treatment with 200 and 400 µM TCEP for 3 days, whereas the lowest concentration of TCEP (100 µM) did not significantly reduce the viability of HepG2 (3.44%). [1]
METHODS: Human peripheral blood mononuclear cell PBMCs were treated with TCEP hydrochloride (0.5-1 mM) for 24 h. Morphological and necrotic changes were assessed by Hoechst 33342/PI staining.
RESULTS: Necrosis was observed in cells treated with 0.5 mM of TCEP. [2] |
| In vivo | METHODS: To investigate the neurotoxicity and its mechanism in mice, TCEP hydrochloride (10-100 mg/kg) was administered by gavage to Kunming mice once a day for 30 days.
RESULTS: Compared with the control group, the water intake of high-dose TCEP group was declined significantly, and the organ index of liver and spleen were increased significantly. In addition, the escape latency of TCEP exposed mice were longer than that in the control group in water maze test, while the total swimming course of high-dose TCEP group was elevated and the swimming time in target quadrant was obviously shortened compared with the control group. TCEP exposure can cause neurotoxicity by increasing thyroid hormones and inducing oxidative damage in mice. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (13.42 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO : 50 mg/mL (134.24 mM)
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| Keywords | TEPP46 | Pyruvate Kinase | TEPP 46 | Inhibitor | inhibit | ML 265 | TEPP-46 | ML-265 |
| Inhibitors Related | DL-Serine | PKM2-IN-1 | PKR-IN-2 | Disodium monofluorophosphate | Shikonin | Mitapivat | PKM2 inhibitor G | DASA-58 | Dimethylaminomicheliolide HCl | PKM2 activator 5 | PKM2 activator 2 |
| Related Compound Libraries | Cuproptosis Compound Library | Glycolysis Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Glutamine Metabolism Compound Library | Anti-Cancer Metabolism Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
United States
