2878360-80-4

2878360-80-4 structure
2878360-80-4 structure
  • Name: MCT1-IN-3
  • Chemical Name: MCT1-IN-3
  • CAS Number: 2878360-80-4
  • Molecular Formula: C22H19N3O4
  • Molecular Weight: 389.40
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monocarboxylate Transporter
  • Create Date: 2023-04-06 16:24:00
  • Modify Date: 2024-01-12 18:57:08
  • MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].

Name MCT1-IN-3
Description MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].
Related Catalog
Target

IC50: 81.0 nM (MCT1)[1] GI50: 20 μM (A-549); 15.1 μM (MCF-7)[1]

In Vitro MCT1-IN-3 (compound 24) 对 MCT1 具有抑制活性,IC50 值为 81.0 nM[1]。 MCT1-IN-3 对表达 MCT1 的癌细胞系 A-549 和 MCF-7 具有很强的抗增殖活性,GI50 值分别为 20 μM 和 15.1 μM[1]< /sup>. MCT1-IN-3(5 μM;24 h)导致癌细胞周期停滞和细胞凋亡[1]。 MCT1-IN-3(1.0、2.0、3.5 和 5.0 μM)显示可使这些癌细胞对抗肿瘤药物敏感[1]。 MCT1-IN-3 还对多药转运蛋白 ABCB1 具有显著的抑制作用,并显示可逆转 ABCB1 介导的多药耐药性 (MDR) [1]。 Cell Cycle Analysis[1] Cell Line: A-549 cells Concentration: 5 μM Incubation Time: 24 h Result: Caused a disruption of the cell cycle of A-549 cancer cells, indicated by a shift from the predominant Go/G, phase. Apoptosis Analysis[1] Cell Line: A-549 cells Concentration: 5 μM Incubation Time: 24 h Result: Increased the percentage of total apoptotic cells by a factor of 13 from 0.51 to 6.68%.
References

[1]. Sachin Puri, et al. Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1). J Med Chem. 2023 Jan 12;66(1):657-676.  

Molecular Formula C22H19N3O4
Molecular Weight 389.40