1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. Monocarboxylate Transporter

Monocarboxylate Transporter (单羧酸转运蛋白)

单羧酸转运蛋白 (MCT) 构成质子连接的质膜转运蛋白家族,其携带具有一个羧酸基团(单羧酸)的分子,例如乳酸和丙酮酸,穿过生物膜。高度恶性的肿瘤严重依赖有氧糖酵解(即使在充足的组织氧气下,葡萄糖也会代谢为乳酸;瓦博格效应),因此需要通过 MCT 将乳酸外排到肿瘤微环境中,以维持强劲的糖酵解通量并防止肿瘤“被腌制致死”。在临床前研究中,使用 RNAi 和小分子抑制剂 α-氰基-4-羟基肉桂酸 (ACCA;CHC) 成功靶向 MCT,表明抑制乳酸外排是治疗高度糖酵解恶性肿瘤的一种非常有效的治疗策略。

Monocarboxylate transporters (MCTs) constitute a family of proton-linked plasma membrane transporters that carry molecules having one carboxylate group (monocarboxylates), such aslactate and pyruvate, across biological membranes. Highly malignant tumors rely heavily on aerobic glycolysis (metabolism of glucose to lactic acid even under ample tissue oxygen; Warburg Effect) and thus need to efflux lactic acid via MCTs to the tumor micro-environment to maintain a robust glycolytic flux and to prevent the tumor from being "pickled to death". The MCTs have been successfully targeted in pre-clinical studies using RNAi and a small-molecule inhibitor alpha-cyano-4-hydroxycinnamic acid (ACCA; CHC) to show that inhibiting lactic acid efflux is a very effective therapeutic strategy against highly glycolytic malignant tumors.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114602
    AR-C117977 Inhibitor
    AR-C117977 是一种有效的单羧酸转运蛋白 (monocarboxylate transporter (MCT1)) 抑制剂。AR-C117977 可延长皮肤和心脏移植物的存活时间。AR-C117977 可部分抑制主动脉移植中移植动脉硬化的发展,但无法抑制移植后的同种抗体产生。AR-C117977 在体内表现出有效的免疫抑制特性,可有效预防小鼠急性而非慢性的移植排斥。
    AR-C117977
  • HY-155382
    Lactate transportor 1
    Lactate transportor 1 (compound 1) 是活细胞中活性的 lactate transporter。Lactate transportor 1 在 Hela、CAL27、MCF7 和 MCF10A 细胞中显示出毒性作用中,IC50 值分别为 3.36、3.27、5.58 和 7.66 μM。Lactate transportor 1 与 Cisplatin (HY-17394) 在 HeLa 细胞中具有叠加效应。
    Lactate transportor 1
  • HY-N0647R
    Silychristin (Standard)

    水飞蓟汀 (Standard)

    Silychristin (Standard) 是 Silychristin 的分析标准品。本产品用于研究及分析应用。Silychristin 是水飞蓟果实中富含的黄酮类化合物,具有抗氧化作用。Silychristin 是甲状腺激素转运体 MCT8 的有效抑制剂,能强烈抑制 T3 的摄取,IC50 为 110 nM。
    Silychristin (Standard)

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