1. Metabolic Enzyme/Protease
  2. Pyruvate Kinase
  3. PKM2-IN-1

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
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10 mg USD 144 In-stock
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50 mg USD 504 In-stock
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100 mg USD 780 In-stock
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200 mg USD 1080 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (16.09 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8945 mL 14.4726 mL 28.9452 mL
5 mM 0.5789 mL 2.8945 mL 5.7890 mL
10 mM 0.2895 mL 1.4473 mL 2.8945 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.56 mg/mL (1.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Product Name:
PKM2-IN-1
Cat. No.:
HY-103617
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