GlpBio

Monocarboxylate Transporters

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.

Monocarboxylate Transporters 相关产品(12)

  • GC10680 structure
    GC10680AR-C155858
    CAS: 496791-37-8
    纯度: >98.00%

    AR-C155858是一种强效的单羧酸转运蛋白1（MCT1）抑制剂，K i 值为2.3nM，也能抑制MCT2，K i 值>10nM。

  • GC10877 structure
    GC10877CHC
    CAS: 28166-41-8
    纯度: >98.00%

    An MCT1 inhibitor

  • GC11010 structure
    GC11010AZD 3965
    CAS: 1448671-31-5
    纯度: >99.50% / >98.00%

    MCT1 的 Ki = 1.6 nMAZD 3965 是单羧酸转运蛋白 1 (MCT1) 的有效抑制剂。

  • GC13691 structure
    GC136917ACC1
    CAS: 50995-74-9
    纯度: >99.50%

    A fluorescent probe

  • GC14642 structure
    GC146427ACC2
    CAS: 1472624-85-3
    纯度: >98.00%

    An MCT1 and MPC inhibitor

  • GC19488 structure
    GC19488BAY-8002
    CAS: 724440-27-1

    An inhibitor of MCT1

  • GC50163 structure
    GC50163SR 13800
    CAS: 227321-12-2
    纯度: >99.00%

    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。

  • GC50226 structure
    GC50226AR-C 141990 hydrochloride
    CAS: 2250019-94-2
    纯度: >98.00%

    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。

  • GC63062 structure
    GC63062MCT4-IN-1
    CAS: 2445185-57-7
    纯度: >98.00%

    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。

  • GC63496 structure
    GC63496VB124
    CAS: 2230186-18-0
    纯度: >99.00%

    VB124是一种安全有效、具有口服活性的选择性单羧酸盐转运蛋白4(MCT4) 抑制剂，VB124阻断了MDA-MB-231细胞中的乳酸输入（IC 50 = 8.6nM）和输出（IC 50 = 19nM）。

  • GC68713 structure
    GC68713AZD0095
    CAS: 2750001-23-9
    纯度: >99.50%

    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。

  • GC73305 structure
    GC73305MCT-IN-1
    CAS: 1685273-57-7
    纯度: >98.00%

    MCT-IN-1（化合物2）是一种强效的单羧酸转运蛋白（MCT）抑制剂，对MCT1和MCT4的IC50分别为9 nM和14 nM。