1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. PDHK

PDHK (丙酮酸脱氢酶激酶)

Pyruvate dehydrogenase (PDH) is a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDH kinase; PDHK; PDK) results in inactivation. Multiple alternatively spliced transcript variants have been found for this gene. PDH catalyzes the conversion of pyruvate to acetyl-coenzyme A, which enters into the Krebs cycle, providing ATP to the cell. PDH activity is under the control of pyruvate dehydrogenase kinases (PDHKs).

PDHK 相关产品 (7):

Cat. No. Product Name Effect Purity
  • HY-Y0445A
    Sodium dichloroacetate Inhibitor ≥98.0%
    Sodium dichloroacetate 是癌细胞线粒体中的一种代谢调节剂,具有抗癌活性。Sodium dichloroacetate 抑制丙酮酸脱氢酶激酶 (PDHK),从而导致肿瘤微环境中的乳酸减少。Sodium dichloroacetate 增加活性氧 (ROS) 的产生并促进癌细胞凋亡,还可作为 NKCC 抑制剂。
  • HY-12492
    VER-246608 Inhibitor 98.92%
    VER-246608 是一种有效的,ATP 竞争性的丙酮酸脱氢酶激酶 (PDK) 抑制剂,抑制 PDK-1PDK-3PDK-2,和 PDK-4IC50 分别为 35 nM,40 nM,84 nM 和 91 nM。
  • HY-16082
    AZD7545 Inhibitor 99.91%
    AZD7545 是一种有效,竞争性和选择性的 PDHK2 抑制剂,对 PDHK1PDHK2IC50 分别为 36.8 nM 和 6.4 nM。
  • HY-N0645
    Dicoumarol Inhibitor ≥98.0%
    Dicoumarol 是 NAD(P)H: 醌氧化还原酶 1 (NQO1) 和 PDK1 的抑制剂,IC50 值分别为 0.37 和 19.42 μM。
  • HY-114702
    M77976 Inhibitor 99.63%
    M77976 是一种特异性的,ATP 竞争性的丙酮酸脱氢酶激酶 PDK4 抑制剂,其作用的 IC50 值为 648 μM。M77976 有用于肥胖症和糖尿病研究的潜力。
  • HY-19564
    JX06 Inhibitor 99.88%
    JX06 是一种有效的,选择性的,共价的 PDK 抑制剂。JX06 抑制 PDK1, PDK2PDK3IC50 值分别为 49 nM,101 nM 和 313 nM。JX06 以不可逆的方式与半胱氨酸残基共价结合来抑制 PDK1 活性。JX06 具有抗肿瘤活性。
  • HY-135954A
    PDK4-IN-1 hydrochloride Inhibitor 99.48%
    PDK4-IN-1 hydrochloride 是一种蒽醌衍生物,也是一种有效的,口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂,IC50 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病,抗癌和抗过敏作用。
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