PKM2 activator 2

PKM2 activator 2 是一种具有抗增殖作用的丙酮酸激酶 M2 (PKM2) 激活剂，AC50 为 66 nM。PKM2 activator 2 可能具有抗肿瘤增殖作用，并缓解 Warburg 效应，因为 PKM2 激活可使细胞恢复正常糖酵解代谢状态。

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5mg

￥1625.00

1300.00

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10mg

￥2725.00

2180.00

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25mg

￥5937.00

4750.00

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50mg

￥9175.00

7340.00

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100mg

￥14425.00

11540.00

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货号: ajcf21122
CAS: 1186660-06-9
别名:
分子式: C20H18F2N2O4S2
分子量: 452.49
纯度: >98%
溶解度: DMSO : 5 mg/mL (11.05 mM; ultrasonic and warming and heat to 60°C)
储存: Store at -20°C
库存: 现货

Background

PKM2 activator 2 is a pyruvate kinase M2 (PKM2) activitor with an AC₅₀ value of 66 nM. PKM2 activator 2 may show anti-tumor proliferation effect and relieve the Warburg effect, while PKM2 activation can restore normal glycolytic metabolism in cells^[1].

PKM2 leads to increased availability of glycolyctic intermediates for biosynthesis of amino acids, nucleic acids, and lipid building blocks for cellular construction in cancer cells. However, PKM2 shows down-regulated expression and dimeric form in tumors and cancer cell lines ^[1].
PKM2 activator 2 (compound 28) is a highly potent activator, activates pyruvate kinase with an AC₅₀ value of 66 nM in the luciferase-coupled assay^[1].

[1]. Boxer MB, et al. Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem. 2010 Feb 11;53(3):1048-55.