| Name | PKM2-IN-1 |
| Description | PKM2-IN-1 (compound 3k) exhibits inhibitory activity against PKM2 with an IC50 of 2.95 μM, while the IC50 for PKM1 is 4-5 times higher. |
| Cell Research | Cell lines (HCT116, Hela, H1299, BEAS-2B) are cultured in RPMI 1640 containing 9% fetal bovine serum (FBS) at 37°C in 5% CO2. Cell viability is detected with the MTS assay according to the manufacturer's instructions. 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 (including PKM2-IN-1) or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3 h. The 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. |
| In vitro | Results show that most of the tested compounds exhibit some degree of PKM2 inhibition and some compounds, such as PKM2-IN-1 (compound 3k) and 6d, display more potent activity than the positive control shikonin. The representative compounds PKM2-IN-1, 6d display dose-dependent inhibition of PKM2 with less inhibition of PKM1 and PKL like shikonin. Among all tested compounds, the most potent compounds are 3a, PKM2-IN-1 and 3r, which exhibit IC50 values against HCT116 and Hela cells ranging from 0.39 to 0.41 μM, 0.18 to 0.29 μM and 0.18 to 0.38 μM, respectively. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 1 mg/mL (2.89 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Pyruvate Kinase | PKM2-IN-1 | PKM-2-IN-1 | PKM2IN1 | PKM2 IN 1 | PKM2 | PKM1 | Inhibitor | inhibit |
| Inhibitors Related | DL-Serine | PKR-IN-2 | Disodium monofluorophosphate | Mitapivat | (+)-Shikonin | PKM2 inhibitor G | DASA-58 | Dimethylaminomicheliolide HCl | TEPP-46 | PKM2 activator 5 | PKM2 activator 2 |
| Related Compound Libraries | Cuproptosis Compound Library | Glycometabolism Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Glutamine Metabolism Compound Library | Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
