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

Monocarboxylate Transporter

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 (5):

Cat. No. Product Name Effect Purity
  • 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-D0067
    7ACC1 Inhibitor 99.66%
    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-D0713
    7ACC2 Inhibitor 99.44%
    7ACC2是MCT高效抑制剂,对[14C]-乳酸流入抑制的IC50值为11nM,是针对癌细胞乳酸转运的新型抗肿瘤分子。
  • 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。
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