A PKM2 inhibitor
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PKM2 Inhibitor

Item No. 36815

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-piperidinecarbodithioic acid, (1,4-dihydro-3-methyl-1,4-dioxo-2-naphthalenyl)methyl ester
CAS Number
94164-88-2
Synonyms
  • Compound 3K
  • MDK4882
  • PKM2-IN-1
  • Pyruvate Kinase M2 Inhibitor
Molecular Formula
C18H19NO2S2
Formula Weight
345.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/ml
SMILES
O=C1C2=C(C(C(CSC(N3CCCCC3)=S)=C1C)=O)C=CC=C2
InChi Code
InChI=1S/C18H19NO2S2/c1-12-15(11-23-18(22)19-9-5-2-6-10-19)17(21)14-8-4-3-7-13(14)16(12)20/h3-4,7-8H,2,5-6,9-11H2,1H3
InChi Key
STAFOGVMELKGRI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

    $160

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    Product Description

    PKM2 inhibitor is an inhibitor of pyruvate kinase M2 (PKM2; IC50 = 2.95 µM), a tumor-specific kinase with a role in glycolysis.1 It is selective for PKM2 over PKM1 and L-type pyruvate kinase (PKLR; IC50s = 16.71 and 8.2 µM, respectively). PKM2 inhibitor is cytotoxic to HCT116, HeLa, and H1299 cells (IC50s = 0.18, 0.29, and 1.56 µM, respectively). It induces apoptosis and autophagy in SKOV3 ovarian cancer cells when used at concentrations of 1, 2.5, and 5 µM.2 In vivo, PMK2 inhibitor (5 mg/kg) reduces tumor volume and weight in an SKOV3 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ning, X., Qi, H., Li, R., et al. Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase. Eur. J. Med. Chem. 138, 343-352 (2017).

    2. Park, J.H., Kundu, A., Lee, S.H., et al. Specific Pyruvate Kinase M2 Inhibitor, Compound 3K, Induces Autophagic Cell Death through Disruption of the Glycolysis Pathway in Ovarian Cancer Cells. Int. J. Biol. Sci. 17(8), 1895-1908 (2021).