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Monocarboxylate Transporters

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.

  1. Cat.No. Product Name Information
  2. GC13691 7ACC1 MCT inhibitor
  3. GC14642 7ACC2 MCT inhibitor
  4. GC50226 AR-C 141990 hydrochloride MCT1 inhibitor
  5. GC10680 AR-C155858

    MCT1 and MCT2 inhibitor

  6. GC11010 AZD 3965 potent inhibitor of monocarboxylate transporter 1 (MCT1)
  7. GC19488 BAY-8002

    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1)

  8. GC10877 CHC Monocarboxylic acid transport (MCT) inhibitor
  9. GC63062 MCT4-IN-1 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。
  10. GC50163 SR 13800 Potent MCT1 inhibitor
  11. GC63496 VB124 VB124 是一种具有口服活性的、有效的、选择性的 MCT4 抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸涌入和流出,IC50 分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。

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