1. Membrane Transporter/Ion Channel
  2. 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 99.67%
    AZD3965 是一种选择性的 MCT1 抑制剂,抑制 MCT1,Ki 为 1.6 nM。比作用于 MCT2 选择性高 6 倍,浓度高达 10 μM,也不抑制 MCT3 和 4。
  • HY-13248
    AR-C155858 Inhibitor
    AR-C155858 是一种新颖的单羧酸转运蛋白 (MCTs) 抑制剂,能够抑制 MCT1 和 MCT2 的活性,Ki 值分别为 2.3 和 < 10 nM;AR-C155858 对 MCT4 没有作用。
  • HY-15475
    UK-5099 Inhibitor 99.57%
    UK-5099是线粒体丙酮酸转运蛋白(MPC)的有效抑制剂, 抑制丙酮酸依赖性O2消耗的IC50值为50 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 99.93%
    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。