1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. Monocarboxylate Transporter
  4. MCT4 Isoform

MCT4

Monocarboxylate transporter 4 (MCT4) also known as solute carrier family 16 member 3 (SLC16A3). MCT4 acts as an H+/lactate exporter in highly glycolytic tissues. In fact, MCT4 was first identified as a key component of lactate efflux in highly glycolytic white fiber myocytes, and was later demonstrated to show a high affinity for lactate over other monocarboxylates, as referenced by its comparatively lower Km for lactate. Furthermore, MCT4 has been shown to be overexpressed in diverse types of neoplasia, among malignant gliomas. Mechanistically, MCT4 is upregulated under hypoxia via binding of HIF-1α to two hypoxic response elements (HRE) within the SLC16A3 promoter. This process enables tumor cells, including those within the core of the heterogeneous tumor mass to survive, despite being at a distance from blood vessels that supply their metabolic needs.

MCT4 相关产品 (3):

目录号 产品名 作用方式 纯度
  • HY-N4115
    Syrosingopine Inhibitor 99.30%
    Syrosingopine (Su 3118) 是一种口服有效的乳酸转运蛋白 MCT1/MCT4 双重抑制剂,可减少糖酵解并可与二甲双胍联合后诱导癌细胞的合成致死性。Syrosingopine 可通过耗损去甲肾上腺素显示抗高血压活性。
  • HY-148517
    AZD0095 Inhibitor 99.59%
    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 (HY-10205) 联合使用可有效抑制 NCI-H358 移植瘤的肿瘤生长。
  • HY-132301
    MSC-4381 Inhibitor 98.11%
    MSC-4381 (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。MSC-4381 靶向与 MCT4 的胞质域。MSC-4381 导致高表达 MCT4 细胞中乳酸流出的抑制和细胞活力的降低。MSC-4381 具有用于 MCT4 转运蛋白研究的潜力。