94164-88-2
94164-88-2 structure
- Name: PKM2-IN-1
- Chemical Name: PKM2 inhibitor
- CAS Number: 94164-88-2
- Molecular Formula: C18H19NO2S2
- Molecular Weight: 345.48
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Pyruvate Kinase
- Create Date: 2018-05-31 13:26:55
- Modify Date: 2024-01-08 19:33:16
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PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
| Name | PKM2 inhibitor |
|---|---|
| Synonyms | PKM2-IN-1 |
| Description | PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 2.95 μM (PKM2)[1] |
| In Vitro | PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95±0.53 μM. 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[1]. |
| Cell Assay | 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. 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[1]. |
| References |
| Molecular Formula | C18H19NO2S2 |
|---|---|
| Molecular Weight | 345.48 |
| Storage condition | -20℃ |