1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. ATP Citrate Lyase

ATP Citrate Lyase (ATP柠檬酸裂解酶)

ATP-citrate lyase (ACLY) is a central metabolic enzyme and catalyses the ATP-dependent conversion of citrate and coenzyme A (CoA) to oxaloacetate and acetyl-CoA. The acetyl-CoA product is crucial for the metabolism of fatty acids, the biosynthesis of cholesterol, and the acetylation and prenylation of proteins. Acetyl CoA is also required for acetylation reactions that modify proteins, such as histone acetylation. ACLY is upregulated or activated in several types of cancers, and its inhibition is known to induce proliferation arrest in cancer cells both in vitro and in vivo.

ACLY links glucose and lipid metabolism by catalyzing the formation of acetyl-CoA and oxaloacetate from citrate produced by glycolysis in the presence of ATP and CoA. ACLY is aberrantly expressed in many immortalized cells and tumors, such as breast, liver, colon, lung and prostate cancers, and is correlated reversely with tumor stage and differentiation, serving as a negative prognostic marker. ACLY is an upstream enzyme of the long chain fatty acid synthesis, providing acetyl-CoA as an essential component of the fatty acid synthesis. Therefore, ACLY is a key enzyme of cellular lipogenesis and potent target for cancer therapy.

ATP Citrate Lyase 相关产品 (9):

目录号 产品名 作用方式 纯度
  • HY-16450
    SB 204990 Inhibitor ≥98.0%
    SB 204990是ATP柠檬酸裂解酶 (ACLY) 的有效特异性抑制剂。
  • HY-16107
    BMS-303141 Inhibitor 98.47%
    BMS-303141是高效性和可渗透细胞的 ACL 抑制剂,IC50值为0.13 μM。
  • HY-12357
    Bempedoic acid Inhibitor ≥98.0%
    Bempedoic acid (ETC-1002) 是一种 ATP-柠檬酸裂解酶 (ATP-citrate lyase;ACL) 抑制剂。Bempedoic acid (ETC-1002) 激活 AMPK
  • HY-127111
    NDI-091143 Inhibitor 99.72%
    NDI-091143 是一种有效的高亲和力人 ATP 柠檬酸裂解酶 (ACLY) 抑制剂,IC50 为 2.1 nM (ADP-Glo分析),Ki 为 7.0 nM,Kd 为 2.2 nM。NDI-091143 通过稳定柠檬酸盐域中的大构象变化来间接抑制柠檬酸的结合和识别,从而抑制了 ACLY 催化变构反应。
  • HY-W009156
    Hydroxycitric acid tripotassium hydrate Inhibitor ≥98.0%
    Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) 是藤黄果的主要活性成分,也是柠檬酸的衍生物。Hydroxycitric acid tripotassium hydrate 可竞争性抑制柠檬酸裂解酶 (ATP citrate lyase) ,并具有减肥效果。Hydroxycitric acid tripotassium hydrate 有效抑制结石形成并抑制 HIF,具有抗氧化,抗炎和抗肿瘤作用。
  • HY-16007
    (-)-Hydroxycitric acid Inhibitor ≥98.0%
    (-)-Hydroxycitric acid (Garcinia acid) 是 Garcinia cambogia 果皮中的主要酸。(-)-Hydroxycitric acid 是一种有效的竞争性 ATP 柠檬酸裂解酶 (ATP citrate lyase) 抑制剂。(-)-Hydroxycitric acid 可抑制脂肪酸的合成,脂肪生成,食物摄入,并促进体重减轻。
  • HY-W012946
    2-Furoic acid Inhibitor ≥98.0%
    2-Furoic acid (Furan-2-carboxylic acid) 是一种有机化合物,经糠醛氧化得到。在大鼠试验中,2-Furoic acid 具有抗血脂作用,能够降低血清中胆固醇和甘油三酯的水平。
  • HY-N7347
    (-)-Hydroxycitric acid lactone Inhibitor
    (-)-Hydroxycitric acid lactone (Garcinia lactone) 是一种减肥药,也是一种很受欢迎的减肥食品补充剂。(-)-Hydroxycitric acid lactone 是一种有效的 ATP-柠檬酸裂解酶 抑制剂。(-)-Hydroxycitric acid lactone 催化柠檬酸盐线粒体外裂解为草酰乙酸和乙酰辅酶 A,限制了脂肪酸合成所需乙酰辅酶 A 单位的可用性。
  • HY-P1123
    MEDICA16 Inhibitor
    MEDICA16 是一种 ATP-citrate lyase 抑制剂,能显著降低腓肠肌细胞内 TG 的含量,这种降低伴随着胰岛素敏感性的增加。MEDICA16 是 GPR40 的选择性激动剂,也是 GPR120 的选择性部分激动剂。
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