Monocarboxylate transporters (MCT)
-
MCT1 inhibitor
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
了解更多
-
MCT1 and MCT2 抑制剂
AR-C155858是单羧酸转运蛋白mct1和mct2的有效抑制剂,它们与涉及跨膜螺旋7-10的细胞内位点结合。
了解更多
- Charlotte Petersen, .et al. MCT1 and MCT4 Expression and Lactate Flux Activity Increase During White and Brown Adipogenesis and Impact Adipocyte Metabolism, Sci Rep, 2017, 7: 13101 PMID: 29026134
- Kong SC, .et al. Monocarboxylate Transporters MCT1 and MCT4 Regulate Migration and Invasion of Pancreatic Ductal Adenocarcinoma Cells, Pancreas, 2016, Aug;45(7):1036-47 PMID: 26765963
- Anne Poder, .et al. Roles of acid-extruding ion transporters in regulation of breast cancer cell growth in a 3-dimensional microenvironment, Mol Cancer, 2016, 15: 45 PMID: 27266704
- Eumorphia G. Konstantakou, .et al. 3-BrPA eliminates human bladder cancer cells with highly oncogenic signatures via engagement of specific death programs and perturbation of multiple signaling and metabolic determinants, Mol Cancer, 2015, 14: 135 PMID: 26198749
- Álvarez Z, .et al. Neurogenesis and vascularization of the damaged brain using a lactate-releasing biomimetic scaffold., Biomaterials., 2014, 35(17):4769-81 PMID: 24636215
- Álvarez Z, .et al. Neuronal Progenitor Maintenance Requires Lactate Metabolism and PEPCK-M-Directed Cataplerosis., Cereb Cortex., 2014, 26(3):1046-58 PMID: 25452568
-
MCT 抑制剂
CHC是单羧酸转运(MCT)抑制剂。在神经胶质瘤中具有抗肿瘤和抗血管生成活性;降低U251细胞的糖酵解代谢,迁移和侵袭。
了解更多
-
MCT1 抑制剂
AZD-3965(AZD3965)是具有1.6 nM结合亲和力的单羧酸盐转运蛋白1(MCT1)的选择性抑制剂,是MCT2的6倍选择性,在10μM时不抑制MCT4。
了解更多
- Lu Gao, .et al. Trophoblast-derived Lactic Acid Orchestrates Decidual Macrophage Differentiation via SRC/LDHA Signaling in Early Pregnancy, Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
-
MCT1 抑制剂
AR-C117977是一种有效的MCT1抑制剂,可以降低体内和体外的免疫应答,维持长期移植物存活,并诱导操作耐受性。
了解更多
-
MCT 抑制剂
7ACC2是一种新型有效的MCT抑制剂,IC50为11 nM,可抑制[14C]-乳酸盐涌入。针对癌细胞中乳酸转运的新型抗肿瘤治疗。
了解更多
-
MCT 抑制剂?
7ACC1在富含乳酸的肿瘤微环境中选择性干扰乳酸通量;在表达MCT1和MCT4转运蛋白的肿瘤细胞中,乳酸抑制乳酸盐流入,但不流出。
了解更多
- Daniel Gundel, .et al. Preclinical Evaluation of [18F]FACH in Healthy Mice and Piglets: An 18F-Labeled Ligand for Imaging of Monocarboxylate Transporters with PET, Int J Mol Sci, 2021, Feb; 22(4): 1645 PMID: 33562048
-
MCT 抑制剂
UK 5099是质膜单羧酸盐转运蛋白(MCT)和线粒体丙酮酸载体(MPC)的有效抑制剂。抑制丙酮酸依赖性的氧气消耗,IC50为50 nM。
了解更多