1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  2. Pyruvate Kinase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin
  3. PKM2-IN-11

PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer.

For research use only. We do not sell to patients.

PKM2-IN-11

PKM2-IN-11 Chemical Structure

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Description

PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer[1].

IC50 & Target

PKM2

0.363 μM (IC50)

In Vitro

PKM2-IN-11 (Compound 30o) (1-25 μM, 24 h) exhibits potent antiproliferative activity (IC50 = 10.2 μM) against MCF-7 cells and shows no cytotoxic effect on HEK-293 cells[1].
PKM2-IN-11 (1-5 μM) results in a dose-dependent decrease in PKM2 protein levels in MCF-7 cells[1].
PKM2-IN-11 (5 μM) increases the microtubule polymerization rate (Vmax) and stabilizes microtubule growth[1].
PKM2-IN-11 slightly reduces ROS levels and induces mitochondrial membrane potential (ΔΨm) depolarization, resulting in a decrease in the red/green fluorescence ratio in MCF-7 cells[1].
PKM2-IN-11 (5 μM) induces a significant increase in early apoptotic cells, with a low proportion of late apoptotic cells, and leads to G2/M phase arrest (23 %) in MCF-7 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM, 10 μM, 25 μM
Incubation Time: 24 h
Result: Exhibited potent antiproliferative activity (IC50 = 10.2 ± 0.07 μM) against MCF-7 cells.
Molecular Weight

462.28

Formula

C21H19IO4

SMILES

CC1(C)C=CC2=C(C=CC(/C=C/C(C3=CC=C(OC)C(I)=C3)=O)=C2O)O1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PKM2-IN-11
Cat. No.:
HY-178441
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