PKM2 inhibitor(compound 3k)

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CAS NO:

94164-88-2

包装与价格：

包装	价格(元)
5mg	电议
25mg	电议

产品介绍

化学性质

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
Canonical SMILES	CC1=C(CSC(N2CCCCC2)=S)C(C3=CC=CC=C3C1=O)=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

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.