Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor. It could rescue the antiproliferative actions of AICAR and metformin. Moreover, dorsomorphin (Compound C) is also used as a selective inhibitor of the BMP pathway. Compound C could inhibit a number of kinases other than AMPK.[1]
In vitro experiments indicate that Compound C inhibits AMPK activity and proliferation of human glioma cells. Dorsomorphin (Compound C) also reduces the apoptosis of cells induced by cisplatin, and decreases the expression of c-caspase3 and c-PARP in cisplatin treatment.
In vivo study demonstrate compound C attenuates cisplatin-induced nephrotoxicity in mice, and alleviates c-caspase 3 and c-PARP induced by cisplatin in kidney tissues.[1][2]
References:
[1].Liu X, et al. The AMPK inhibitor compound C is a potent AMPK-independent antiglioma agent. Mol Cancer Ther. 2014 Mar;13(3):596-605.
[2].Li F, et al. Compound C Protects Against Cisplatin-Induced Nephrotoxicity Through Pleiotropic Effects. Front Physiol. 2020 Dec 23;11:614244.
Dorsomorphin（Compound C）是一种细胞渗透的AMPK抑制剂。它可以挽救AICAR和二甲双胍的抗增殖作用。此外,dorsomorphin（Compound C）还被用作BMP通路的选择性抑制剂。 Compound C除了能够抑制AMPK之外,还能够抑制其他多种激酶。 [1]
体外实验表明,复合物C抑制AMPK活性和人脑胶质瘤细胞的增殖。Dorsomorphin（复合物C）还减少了顺铂诱导的细胞凋亡,并降低了顺铂治疗中c-caspase3和c-PARP的表达。
动物实验表明,化合物C可以减轻小鼠因顺铂引起的肾毒性,并且缓解了顺铂在肾脏组织中引起的c-caspase 3和c-PARP。[1][2]