PKM2-IN-1

This product is for research use only, not for human use. We do not sell to patients.

PKM2-IN-1
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250mg$750Check With Us
500mg$1200Check With Us
1g$1800Check With Us

Cat #: V3420 CAS #: 94164-88-2 Purity ≥ 98%

Description: PKM2-IN-1 is a novel and potent inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 2.95 μM.

References: 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.

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Molecular Weight (MW)345.48
Molecular FormulaC18H19NO2S2
CAS No.94164-88-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeO=C1C(CSC(N2CCCCC2)=S)=C(C)C(C3=CC=CC=C31)=O
SynonymsPKM2 inhibitor; MDK4882; MDK-4882; MDK 4882; compound 3k; PKM2-IN-1
ProtocolIn VitroPKM2-IN-1 (compound 3k) 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.8945 mL14.4726 mL28.9452 mL57.8905 mL
5mM0.5789 mL2.8945 mL5.7890 mL11.5781 mL
10mM0.2895 mL1.4473 mL2.8945 mL5.7890 mL
20mM0.1447 mL0.7236 mL1.4473 mL2.8945 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.