Monocarboxylate Transporters(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.

Cat.No. 产品名称 Information
GC68713 AZD0095 AZD0095 是一种具有选择性和口服活性的 MCT4 抑制剂 (IC50: 1.3 nM)。 AZD0095 与 Cediranib 联合使用可有效抑制 NCI-H358 移植瘤的肿瘤生长。
GC63496 VB124 VB124, a potent and selective MCT4 inhibitor, specifically inhibits lactate efflux/import in MDA-MB-231 cells expressing MCT4, and is used for the research of cardiac hypertrophy, heart failure, and metabolism.
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。
GC50226 AR-C 141990 hydrochloride AR-C 141990 hydrochloride 是一种有效的乳酸转运蛋白（单羧酸转运蛋白；MCTs）抑制剂，MCT-1 和 MCT-2 的 pKi 值分别为 7.6 和 6.6。
GC50163 SR 13800 SR 13800 是一种有效的单羧酸转运蛋白 1 (MCT1) 抑制剂。 SR 13800 具有抗癌活性。
GC19488 BAY-8002 An inhibitor of MCT1
GC11010 AZD 3965 A selective inhibitor of MCT1
GC14642 7ACC2 An MCT1 and MPC inhibitor
GC13691 7ACC1 A fluorescent probe
GC10877 CHC An MCT1 inhibitor
GC10680 AR-C155858 An inhibitor of MCT1 and 2