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PKM2 inhibitor(compound 3k)

Catalog No.
B8217
A potent, selective PKM2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$80.00
In stock
25mg
$240.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PKM2 inhibitor (compound 3k) is a potent, selective inhibitor of pyruvate kinase M2 (PKM2) with the IC50 value of 2.95 μM. PKM2 is a rate-limiting enzyme of the glycolytic pathway which is preferentially expressed in various tumors. Cancer cells rely heavily on PKM2 for aerobic glycolysis, and specific targeting of PKM2 therefore offers a potential strategy for cancer therapy. 

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. European Journal of Medicinal Chemistry, 2017, 138: 343-352.

2. Park JH, Kundu A, Lee SH, et al. Specific pyruvate kinase M2 inhibitor, compound 3k, induces autophagic cell death through disruption of the glycolysis pathway in ovarian cancer cells. International Journal of Biological Sciences, 2021, 17(8): 1895-1908.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt345.48
Cas No.94164-88-2
FormulaC18H19NO2S2
Solubility≥34.5 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O
Chemical Name(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methyl piperidine-1-carbodithioate
SDFDownload SDF
Canonical SMILESCC1=C(CSC(N2CCCCC2)=S)C(C3=CC=CC=C3C1=O)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment:[1]

Cell lines

HCT116, Hela, H1299 and BEAS-2B cells

Reaction Conditions

48 h incubation

Applications

PKM2 inhibitor (compound 3k) showed nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299, with IC50 values of 0.18, 0.29 and 1.56 μM, respectively. Moreover, PKM2 inhibitor (compound 3k) exhibited more cytotoxicity on cancer cells (H1299) than normal cells (BEAS-2B).

Animal experiment:[2]

Animal models

BALB/c nude mice subcutaneously injected with SK-OV-3 cells

Dosage form

5 mg/kg

Administered orally every 2 days for 31 days

Applications

PKM2 inhibitor (compound 3k) treatment markedly decreased the tumor volume and tumor weight, compared with the control group. Meanwhile, no significant weight reduction was detected in the mouse treated with PKM2 inhibitor (compound 3k), suggesting that PKM2 inhibitor (compound 3k) did not cause any major organ toxicity. Thus, use of specific PKM2 inhibitors to block the glycolytic pathway and target cancer cell metabolism represents a promising therapeutic approach for treating PKM2-overexpressing ovarian cancer.

Note

The technical data provided above is for reference only

 

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. European Journal of Medicinal Chemistry, 2017, 138: 343-352.

2. Park JH, Kundu A, Lee SH, et al. Specific pyruvate kinase M2 inhibitor, compound 3k, induces autophagic cell death through disruption of the glycolysis pathway in ovarian cancer cells. International Journal of Biological Sciences, 2021, 17(8): 1895-1908.

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