Solute Carrier Family 25 (SLC25) is the largest family of mitochondrial membrane proteins in the human body, consisting of 53 members. Mitochondrial phosphate carriers (MPiC), cellular iron metabolism, voltage-dependent anion channels (VDAC), and oxidative phosphorylation in the SLC25family play dominant roles in material transport, energy metabolism, etc. SLC25family-related proteins are involved in the regulation of the progression of a variety of cancers, including colon, gastric, and lung cancers. In addition, the SLC25family has been implicated in endoplasmic reticulum stress (ERS) and immunity. Since SLC25family proteins are involved in cancer progression and are associated with endoplasmic reticulum stress and immunity, exploring inhibitors of SLC25family-related proteins is essential. However, the exact mechanism of SLC25family-related proteins involved in cancer, as well as potential targets and SLC25inhibitors have not been reported in the literature. This article focuses on summarizing the relevance of the SLC25family to cancer, ERS, and immunity. This review also provides a comprehensive overview of SLC25family-related inhibitors.