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

Monocarboxylate Transporter (单羧酸转运蛋白)

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.

Monocarboxylate Transporter 相关产品 (9):

目录号 产品名 作用方式 纯度
  • HY-12750
    AZD3965 Inhibitor 99.95%
    AZD3965是选择性的 MCT1 抑制剂,Ki 值为1.6 nM,比MCT2的选择性高6倍。
  • HY-13248
    AR-C155858 Inhibitor
    AR-C155858是选择性的单羧酸转运蛋白 MCT1MCT2 抑制剂,Ki 分别为2.3 nM和10 nM。
  • HY-122312
    BAY-8002 Inhibitor 98.10%
    BAY-8002 是一种有效、选择性、可口服的单羧酸转运蛋白第 1 亚型 (monocarboxylate transporter 1 (MCT1)) 抑制剂,在表达 MCT1 的 DLD-1 细胞中,IC50 值为 85 nM,对 MCT1 的选择性远高于 MCT4。具有抗肿瘤活性。
  • HY-D0713
    7ACC2 Inhibitor 99.80%
    7ACC2 是一种有效的单羧酸盐转运蛋白 (MCT) 抑制剂,IC50 为 11 nM,可抑制乳酸涌入。7ACC2 还是一种线粒体丙酮酸转运 (mitochondrial pyruvate transport) 的有效抑制剂。7ACC2 通过抑制乳酸通量来发挥抗癌作用。
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid Inhibitor ≥98.0%
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) 是有效的非竞争性单羧酸盐转运蛋白 (MCTs) 抑制剂。α-Cyano-4-hydroxycinnamic acid 抑制线粒体丙酮酸转运蛋白,Ki 值为 6.3 μM。α-Cyano-4-hydroxycinnamic acid 用作基质辅助激光解吸电离-飞行时间质谱 (MALDI-TOF) 分析的基质,可以促进肽离子化。
  • HY-132301
    MCT4-IN-1 Inhibitor
    MCT4-IN-1 是一种口服有效的,选择性的单羧酸转运蛋白 4 (MCT4/SLC16A3) 抑制剂,IC50 值为 77 nM,Ki 值为 11 nM。MCT4-IN-1 靶向与 MCT4 的胞质域。MCT4-IN-1 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MCT4-IN-1 具有用于 MCT4 转运蛋白研究的潜力。
  • HY-D0067
    7ACC1 Inhibitor 99.72%
    7ACC1(DEAC; Coumarin D 1421; D 1421)能选择性干扰肿瘤微环境乳酸通量,能抑制表达MCT1和MCT4肿瘤细胞的乳酸涌入,但对乳酸流出无影响。
  • HY-18974
    MCT1-IN-2 Inhibitor
    MCT1-IN-2 是有效的单羧酸盐转运蛋白 1 (MCT1) 抑制剂。MCT1-IN-2 具有抗癌活性。
  • HY-119996A
    AR-C141990 hydrochloride Inhibitor
    AR-C141990 hydrochloride 是一种有效的乳酸转运蛋白 (monocarboxylate transporters; MCTs) 抑制剂,对 MCT-1 和 MCT-2 的 pKi 分别为 7.6、6.6。AR-C141990 hydrochloride 具有免疫抑制特性,可抑制移植物抗宿主反应。
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