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PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2. The well performing PKM2-IN-1 (compound 3k) shows nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18-1.56 μM.
Moreover, PKM2-IN-1 (compound 3k) exhibits more cytotoxicity on cancer cells than normal cells.
| Cell Experiment | |
|---|---|
| Cell lines | HCT116, Hela, H1299, BEAS-2B |
| Preparation method | Cell viability is detected with the MTS assay. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h, the cells are treated with different concentration of tested compound or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3h. Absorbance of each well is determined by a microplate reader at a 490 nm wavelength. The IC50 values are calculated using Prism Graphpad software of the triplicate experiment. |
| Concentrations | 0.078, 0.156, 0.313, 0.625 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 345.48 |
| Formula | C18H19NO2S2 |
| CAS Number | 94164-88-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 7 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Pyruvate Kinase Products |
|---|
| Sodium Monofluorophosphate
Monofluorophosphate is a competitive inhibitor of pyruvate kinase and alkaline phosphatase with Ki of 3.4 mM and 69 μM, respectively, which also irreversibly inhibits phosphorylase phosphatase with Ki of 0.5 mM. |
| TEPP-46
Ml-265 (TEPP-46) is an effective activator of pyruvate kinase M2 (PKM2). ML265 induces the more active tetrameric state of PKM2 and the X-ray co-crystal structure shows that the activator binds at the dimer-dimer interface between two subunits of PKM2. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine. |
| Mitapivat (AG-348)
Mitapivat (AG-348) is the first-in-class, oral effective pyruvate kinase small molecule allosteric activator. Mitapivat (AG-348) is active against wild-type and various mutated PKR enzymes, and promotes healthy red blood cell generation by activating mutated PKR to increase ATP levels. |
| DASA-58
DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC90 of 680 nM, and an AC50 of 38 nM. |
| Etavopivat
Etavopivat, an oral erythrocyte pyruvate kinase activator, is being developed for sickle cell disease and other hemoglobinopathies, previously reported in 2019. |
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