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PKM2-IN-1

Catalog No. T4170   CAS 94164-88-2
Synonyms: PKM2 inhibitor, compound 3k

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PKM2-IN-1 Chemical Structure
PKM2-IN-1, CAS 94164-88-2
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
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Purity: 99.9%
Purity: 99.68%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6 mg/mL (17.36 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Ning X, et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. Eur J Med Chem. 2017 Sep 29;138:343-352.

TargetMolCitations

1. Deng H, Qian X, Zhang Y, et al.Metformin Increases the Response of Cholangiocarcinoma Cells to Gemcitabine by Suppressing Pyruvate Kinase M2 to Activate Mitochondrial Apoptosis.Digestive Diseases and Sciences.2024: 1-15.

Related compound libraries

This product is contained In the following compound libraries:
Target-Focused Phenotypic Screening Library Glutamine Metabolism Compound Library Glycometabolism Compound Library Lipid Metabolism Compound Library Kinase Inhibitor Library Cuproptosis Compound Library Bioactive Compounds Library Max Inhibitor Library Anti-Cancer Metabolism Compound Library Metabolism Compound Library

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Keywords

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

 

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