1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase

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 with unique tissue expression patterns and regulatory properties. Pyruvate kinase has four different tissue-specific isozymes in animals, PKL, PKR, PKM1, and PKM2. The L and R isozymes are expressed in the liver (L) and red blood cells (R), whereas PKM2 is expressed in early embryonic cells and other proliferating cells, and PKM1 is expressed in the brain, skeletal muscle, and heart which need high energy.

PKM1 and PKM2 are formed by a single mRNA transcript of the PKM gene by alternative splicing. The oligomers of PKM2 exist in high activity tetramer and low activity dimer forms. The dimer PKM2 regulates the rate-limiting step of glycolysis that shifts the glucose metabolism from the normal respiratory chain to lactate production in tumor cells. Besides its role as a metabolic regulator, it also acts as a protein kinase, which contributes to tumorigenesis. PKM2 serves as a promising target for cancer treatment.

Pyruvate Kinase 相关产品 (9):

目录号 产品名 作用方式 纯度
  • HY-18657
    TEPP-46 Activator ≥98.0%
    TEPP-46 (ML-265) 是一种有效,选择性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活剂,AC50 值为 92 nM,对 PKM1,PKL 和 PKR 作用较小或没有作用。
  • HY-N0822
    Shikonin Inhibitor 99.80%
    Shikonin 是中草药紫草的主要成分。Shikonin 是一种有效的 TMEM16A 氯化物通道 (chloride channel) 抑制剂,IC50 为 6.5 μM。Shikonin 是一种特异的丙酮酸激酶 M2 (PKM2) 抑制剂,还可以抑制 TNF-αNF-κB途径。Shikonin 通过抑制糖酵解降低外泌体 (exosome) 的分泌。Shikonin 抑制 AIM2炎性体活化。
  • HY-103617
    PKM2-IN-1 Inhibitor
    PKM2-IN-1 是一种丙酮酸激酶 M2 (PKM2) 抑制剂,其 IC50 值为 2.95 μM。
  • HY-19330
    DASA-58 Activator 99.79%
    DASA-58是有效的丙酮酸激酶M2 (PKM2) 活化剂,其中AC90AC50分别为680 nM,38 nM。
  • HY-12689
    Mitapivat Activator 99.85%
    Mitapivat (AG-348) 是一种丙酮酸激酶 M2 型同工酶 (PKM2) 激活剂。
  • HY-139573
    Etavopivat Activator
    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。
  • HY-19702
    PKR-IN-2 Activator 99.97%
    PKR-IN-2 是一种丙酮酸激酶 PKR 亚型的激活剂,提详细信息请参考专利文献 WO2014139144A1 中的化合物 160。PKR-IN-2 可用于 PKR 功能相关疾病的研究,包括癌症、糖尿病、肥胖、自身免疫性疾病、良性前列腺增生等。
  • HY-135884
    PKR activator 2 Activator
    PKR activator 2 是一种有效的丙酮酸激酶 R (PKR) 激活剂,详细信息请参考专利文献 WO2019035863A1 中的化合物 385。
  • HY-135883
    PKR activator 1 Activator
    PKR activator 1 是一种有效的丙酮酸激酶 R (PKR) 激活剂,详细信息请参考专利文献 WO2019035865A1 中的化合物 E7-93。
Isoform Specific Products

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