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TEPP 46

Cat. No. 7809 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective pyruvate kinase M2 (PKM2) allosteric activator
化学名： 6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one
纯度： ≥98% (HPLC)
说明书
引用文献
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for TEPP 46

TEPP 46 is a potent and selective allosteric activator of pyruvate kinase M2 (PKM2) (EC50 = 92 nM); it exhibits no effect on PKM1. TEPP 46 binds at the dimer-dimer interface of the PKM2 homotetramer, blocks its translocation into the nuclues and promotes a constitutively PKM2 active state. TEPP 46 impairs H1299 lung cancer cell proliferation under hypoxic conditions but not under normoxia in vitro. It inhibits growth of H1299 tumor xenografts in mice. TEPP 46 can reverse fructose-derived F1P inhibition of PKM2 and prevent fructose promoted hypoxia adaptation of intestinal cells. TEPP 46 reduces activation, proliferation, and cytokine production of both T helper 17 (Th17) and Th1 cells in vitro. It also inhibits experimental autoimmune encephalomyelitis (EAE) in vivo. Orally bioavailable.

许可信息

Sold under licence from the National Institute of Health.

技术数据 for TEPP 46

分子量 372.47
公式 C17H16N4O2S2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1221186-53-3
PubChem ID 44246499
InChI Key ZWKJWVSEDISQIS-UHFFFAOYSA-N
Smiles O=C1C2=C(C=NN1CC=3C=CC=C(N)C3)C=4SC(=CC4N2C)S(=O)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for TEPP 46

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 37.25 100

制备储备液 for TEPP 46

以下数据基于产品分子量 372.47。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.68 mL 13.42 mL 26.85 mL
5 mM 0.54 mL 2.68 mL 5.37 mL
10 mM 0.27 mL 1.34 mL 2.68 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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参考文献 for TEPP 46

参考文献是支持产品生物活性的出版物。

Anastasiou et al (2012) Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat.Chem.Biol. 8 839 PMID: 22922757

Angiari et al (2020) Pharmacological activation of pyruvate kinase M2 inhibits CD4+ T Cell pathogenicity and suppresses autoimmunity. Cell Metab. 31 391 PMID: 31761564

Taylor et al (2021) Dietary fructose improves intestinal cell survival and nutrient absorption. Nature 597 263 PMID: 34408323

If you know of a relevant reference for TEPP 46, please let us know.

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关键词: TEPP 46, TEPP 46 supplier, TEPP46, potent, selective, allosteric, activator, activates, pyruvate, kinase, M2, PKM2, hypoxia, Other, Kinases, 7809, Tocris Bioscience

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