1. Metabolic Enzyme/Protease
  2. Pyruvate Kinase

PKM2-IN-1 

Cat. No.: HY-103617 Purity: 98.35%
Handling Instructions

PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.

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

PKM2-IN-1 Chemical Structure

PKM2-IN-1 Chemical Structure

CAS No. : 94164-88-2

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.

IC50 & 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].

References
Cell Assay
[1]

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].

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

References
Molecular Weight

345.48

Formula

C₁₈H₁₉NO₂S₂

CAS No.

94164-88-2

SMILES

S=C(N1CCCCC1)SCC(C2=O)=C(C)C(C3=C2C=CC=C3)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PKM2-IN-1
Cat. No.:
HY-103617
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PKM2-IN-1

Cat. No.: HY-103617