Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PKM2-IN-1 (compound 3k) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 47.00 | |
5 mg | In stock | $ 77.00 | |
10 mg | In stock | $ 117.00 | |
25 mg | In stock | $ 216.00 | |
50 mg | In stock | $ 372.00 | |
100 mg | In stock | $ 596.00 | |
200 mg | In stock | $ 852.00 | |
500 mg | In stock | $ 1,280.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 85.00 |
Description | PKM2-IN-1 (compound 3k) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2. |
Targets&IC50 | PKM2:2.95 μM |
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. |
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. |
Synonyms | PKM2 inhibitor, compound 3k |
Molecular Weight | 345.48 |
Formula | C18H19NO2S2 |
CAS No. | 94164-88-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6 mg/mL (17.36 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
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PKM2-IN-1 94164-88-2 Metabolism PKM Pyruvate Kinase inhibit PKM2 IN 1 Inhibitor PKM2 inhibitor PKM2IN1 PKM-2-IN-1 compound 3k inhibitor