gp 2.5

KGP-25,一种电压门控钠通道 1.8 (Nav1.8) 抑制剂,通过靶向周围神经系统 (PNS) 中的 Nav1.8 实现镇痛作用.此外,KGP-25 还能作用于中枢神经系统 (CNS) 中的 γ-氨基丁酸亚型 A 受体 (GABAA),用于全身麻醉.

CGP 25454A is a novel and selective antagonist of the presynaptic dopamine autoreceptor.

P-gp inhibitor 5 是 P 糖蛋白 (P-gp) 的有效抑制剂，在 1.25 μM 和 2.5 μM 时 P-gp 抑制倍数分别为 2.5 和 3.0。P-gp inhibitor 5 对某些癌细胞表现出抗增殖效果。P-gp inhibitor 5 能够恢复细胞对 Vincristine 和 Paclitaxel 的敏感性，进而逆转 ABCB1 Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。

Indium (III) thiosemicarbazone 5b is an anticancer compound demonstrating cytotoxicity against various cancer cell lines including A549, MCF-7 breast, cisplatin-resistant MCF-7/DDP breast, and Hl 7702 liver cancer cells, with IC50 values of 2.41, 1.97, 2.11, and 8.95 µM, respectively. It effectively lowers PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo studies show that at a dosage of 2.5 µmol/kg, indium (III) thiosemicarbazone 5b significantly reduces tumor weight and volume in MCF-7/DDP mouse xenograft models. Furthermore, liposomes formulated with this compound promote apoptosis and pro-death autophagy in MCF-7/DDP cells, alongside notable reductions in tumor volume and weight, showcasing its potential as a therapeutic agent in cancer treatment.