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首页-小分子抑制剂&激动剂-Others-Pyruvate Kinase-Micheliolide
Micheliolide

Chemical Structure : Micheliolide

CAS No.: 68370-47-8

Micheliolide

货号: PC-23535Not For Human Use, Lab Use Only.

Micheliolide (MCL) is a potent, selective and allosteric activator of PKM2, selectively activates pyruvate kinase M2 (PKM2) through the covalent binding at Cys424, effectively promotes the pyruvate kinase activity of rPKM2 with AC50 of 6 nM, shows broad-spectrum anticancer and anti-inflammation activity.

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5 mg ¥1280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Micheliolide (MCL) is a potent, selective and allosteric activator of PKM2, selectively activates pyruvate kinase M2 (PKM2) through the covalent binding at Cys424, effectively promotes the pyruvate kinase activity of rPKM2 with AC50 of 6 nM, shows broad-spectrum anticancer and anti-inflammation activity.
Micheliolide (MCL) selectively inhibits acute myelogenous leukemia stem and progenitor cells.
Micheliolide (MCL) inhibited NF-κB activation and subsequent pro-inflammatory pathways activation in vitro and in vivo.
Micheliolide inhibits LPS-induced inflammatory response and protects mice from LPS challenge.
Micheliolide provides protection of mice against Staphylococcus aureus and MRSA infection by down-regulating inflammatory response.

物理化学性质&存储条件

分子量 248.32
分子式 C15H20O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Azuleno[4,5-b]furan-2(3H)-one, 3a,4,5,7,8,9,9a,9b-octahydro-9-hydroxy-6,9-dimethyl-3-methylene-, (3aS,9R,9aS,9bS)-

参考文献

1. Zhang Q, et al. J Med Chem. 2012 Oct 25;55(20):8757-69.

2. Li J, et al. J Med Chem. 2018 May 10;61(9):4155-4164.

3. Jiang X, et al. Sci Rep. 2017 Feb 6;7:41964.

4. Viennois E, et al. Lab Invest. 2014 Sep;94(9):950-65.

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