PKM2 inhibitor(compound 3k)

製品コードS8616 バッチS861601

印刷

化学情報

Synonyms

PKM2-IN-1

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₉NO₂S₂

分子量

345.48

CAS No.

94164-88-2

Solubility (25°C)*

体外

DMSO

6 mg/mL (17.36 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O	0.5mg/ml	Taking the 1 mL working solution as an example, add 100 μL of 5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95%Corn oil	0.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PKM2 inhibitor(Compound 3K, PKM2-IN-1) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.
in vitro	The well performing compound 3k shows nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18-1.56 μM. Moreover, compound 3k exhibits more cytotoxicity on cancer cells than normal cells^[1].
in vivo	Compound 3K (PKM2-IN-1) is an enzymatic inhibitor of pyruvate kinase M2 (PKM2).

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCT116, Hela, H1299, BEAS-2B
	濃度	0.078, 0.156, 0.313, 0.625 μM
	反応時間	48 h
	実験の流れ	Cell viability is detected with the MTS assay. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h, the cells are treated with different concentration of tested compound or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3h. Absorbance of each well is determined by a microplate reader at a 490 nm wavelength. The IC50 values are calculated using Prism Graphpad software of the triplicate experiment.
動物実験	動物モデル	Male C57BL/6 mice
	投薬量	1.2 μM
	投与方法	Topical

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Transcriptomics of Hirschsprung disease patient-derived enteric neural crest cells reveals a role for oxidative phosphorylation [ Nat Commun, 2023, 14(1):2157]	PubMed: 37061531
Mediation of PKM2-dependent glycolytic and non-glycolytic pathways by ENO2 in head and neck cancer development [ J Exp Clin Cancer Res, 2023, 42(1):1]	PubMed: 36588153
USP11 exacerbates neuronal apoptosis after traumatic brain injury via PKM2-mediated PI3K/AKT signaling pathway [ Brain Res, 2023, 1807:148321]	PubMed: 36898475
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305]	PubMed: 36203054
Long non-coding RNA VAL facilitates PKM2 enzymatic activity to promote glycolysis and malignancy of gastric cancer [ Clin Transl Med, 2022, 12(10):e1088]	PubMed: 36229913
Lactylation of PKM2 Suppresses Inflammatory Metabolic Adaptation in Pro-inflammatory Macrophages [ Int J Biol Sci, 2022, 18(16):6210-6225]	PubMed: 36439872
Novel Specific Pyruvate Kinase M2 Inhibitor, Compound 3h, Induces Apoptosis and Autophagy through Suppressing Akt/mTOR Signaling Pathway in LNCaP Cells [ Cancers (Basel), 2022, 15(1)265]	PubMed: 36612260
Inhibition of abnormally activated HIF-1α-GLUT1/3-glycolysis pathway enhances the sensitivity of hepatocellular carcinoma to 5-caffeoylquinic acid and its derivatives [ Eur J Pharmacol, 2022, S0014-2999(22)00105-4]	PubMed: 35189090
PDGF-BB/PDGFRβ promotes epithelial-mesenchymal transition by affecting PI3K/AKT/mTOR-driven aerobic glycolysis in Wilms' tumor G401 cells [ Cell Biol Int, 2022, 10.1002/cbin.11780]	PubMed: 35165984
The role of NFATc1/c-myc/PKM2/IL-10 axis in activating cervical cancer tumor-associated M2 macrophage polarization to promote cervical cancer progression [ Exp Cell Res, 2022, S0014-4827(22)00045-3]	PubMed: 35122827

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。