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Pyruvate kinase(丙酮酸激酶)

Pyruvate kinase is an enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP in glycolysis and plays a role in regulating cell metabolism. There are four mammalian pyruvate kinase isoforms (PKM1, PKM2, PKR, PKL), and each isoform has had multiple designations over time in the literature. The M2 isoform of pyruvate kinase (PKM2) supports anabolic metabolism and is expressed both in cancer and normal tissue. The enzymatic activity of PKM2 is allosterically regulated by both intracellular signaling pathways and metabolites; PKM2 thus integrates signaling and metabolic inputs to modulate glucose metabolism according to the needs of the cell.

  1. Cat.No. 产品名称 Information
  2. GC64428 Etavopivat Etavopivat 是一种有效的、选择性的、口服生物可利用的红细胞 (RBC) 丙酮酸激酶 (PKR) 激活剂,具有有效的抗镰刀化作用。
  3. GC32738 PKM2-IN-1 PKM2-IN-1 是一种丙酮酸激酶 M2 (PKM2) 抑制剂,IC50 为 2.95 μM。
  4. GC19297 Mitapivat Mitapivat (AG-348) 是一种具有口服活性的丙酮酸激酶变构激活剂。
  5. GC11741 ML-265 ML-265 (ML-265) 是一种有效的选择性丙酮酸激酶 M2 (PKM2) 激活剂,AC50 为 92 nM,对 PKM1、PKL 和 PKR 几乎没有影响。
  6. GC12888 DASA-58 DASA-58 是一种潜在的丙酮酸激酶同工酶 (PKM2) 别构激活剂。
  7. GN10216 Shikonin 紫草素是一种名为紫草的中草药的主要成分。 Shikonin 是一种有效的 TMEM16A 氯离子通道抑制剂,IC50 为 6.5 μM。 Shikonin 是一种特异性丙酮酸激酶 M2 (PKM2) 抑制剂,还可以抑制 TNF-α 和 NF-κB 通路。紫草素通过抑制糖酵解减少外泌体分泌。 Shikonin 抑制 AIM2 炎性体激活。

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