PKM2-IN-1 (Compound 3k)

製品コードS8616 バッチS861601

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
* <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) は、IC50値2.95 μMでPKM2阻害活性を示します。PKM1のIC50値は、PKM2のそれより4〜5倍高いです。
in vitro	The well performing PKM2 inhibitor (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, it exhibits more cytotoxicity on cancer cells than normal cells.
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 after treatment with PKM2 inhibitor (compound 3k). 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 it 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

https://pubmed.ncbi.nlm.nih.gov/28688274/
https://pubmed.ncbi.nlm.nih.gov/36439872/

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：

SRT3025-loaded cell membrane hybrid liposomes (3025@ML) enhanced anti-tumor activity of Oxaliplatin via inhibiting pyruvate kinase M2 and fatty acid synthase [ Lipids Health Dis, 2025, 24(1):14]	PubMed: 39825408
Increasing cisplatin exposure promotes small-cell lung cancer transformation after a shift from glucose metabolism to fatty acid metabolism [ J Cancer Res Clin Oncol, 2025, 151(3):126]	PubMed: 40155472
Context-dependent modification of PFKFB3 in hematopoietic stem cells promotes anaerobic glycolysis and ensures stress hematopoiesis [ Elife, 2024, 12RP87674]	PubMed: 38573813
PKM2-mediated STAT3 phosphorylation promotes acute liver failure via regulating NLRP3-dependent pyroptosis [ Commun Biol, 2024, 7(1):1694]	PubMed: 39722076
TRIM27 promotes the Warburg effect and glioblastoma progression via inhibiting the LKB1/AMPK/mTOR axis [ Am J Cancer Res, 2024, 14(7):3468-3482]	PubMed: 39113875
Muscle-specific pyruvate kinase isoforms, PKM1 and PKM2, regulate mammalian SWI/SNF proteins and histone 3 phosphorylation during myoblast differentiation [ FASEB J, 2024, 38(11):e23702]	PubMed: 38837439
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

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。

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