PKM2 inhibitor(compound 3k)
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 345.48 |
| Cas No. | 94164-88-2 |
| Formula | C18H19NO2S2 |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(CSC(N2CCCCC2)=S)C(C3=CC=CC=C3C1=O)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
HCT116, Hela, H1299 and BEAS-2B cells |
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Reaction Conditions |
48 h incubation |
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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] | |
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Animal models |
BALB/c nude mice subcutaneously injected with SK-OV-3 cells |
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Dosage form |
5 mg/kg Administered orally every 2 days for 31 days |
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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. |
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Note |
The technical data provided above is for reference only |
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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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Quality Control & MSDS
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Chemical structure
