SREBP1/SREBP2 |
Fatostatin |
Prostate cancer |
Inhibits cell proliferation, invasion, and migration of cancer cells and causes G2-M cell cycle arrest and induces apoptosis (Li et al., 2014b) |
Inhibits prostate tumor growth and distant lymph node metastasis in mice by inhibiting the activation of SREBPs (Chen et al., 2018) |
Combined use with docetaxel can inhibit the proliferation and apoptosis of prostate cancer cells (especially p53 mutants) to a greater extent (Li et al., 2015d) |
Endometrial cancer |
Inhibits metabolic signaling pathways regulated by SREBPs and induces caspase-mediated apoptosis (Gao et al., 2018) |
Inhibits growth, proliferation, cell cycle, and apoptosis and has antitumor activity in vivo (Yao et al., 2020) |
Breast cancer |
Causes cell cycle arrest and apoptosis by ER stress (Brovkovych et al., 2018) |
Multiple cancers |
Inhibits tubulin polymerization and mitosis and perturbs its mitotic microtubule spindle assembly (Gholkar et al., 2016) |
Betulin |
Hepatocellular carcinoma |
Reduces the levels of pro-inflammatory lipids and suppresses inflammation and ER stress by inhibiting the translocation of SREBPs (Li et al., 2017) |
Inhibits glucose metabolism and enhances the antitumor effect of Sorafenib by inhibiting SREBP1 (Yin et al., 2019) |
PF-429242 |
Renal cell carcinoma |
Inhibits cell proliferation, migration, and invasion, and activates apoptosis by targeting S1P (Wang et al., 2021b) |
Hepatocellular carcinoma |
Inhibits viral assembly in infected cells by reducing LD formation, thereby blocking HCV establishment of infection (Blanchet et al., 2012; Olmstead et al., 2012) |
Synergizes with GSK343, enhancing the anticancer activity of GSK343 (Yang et al., 2019) |
Glioblastoma |
Downregulates steroid, isoprenoid, and unsaturated fatty acid biosynthetic signaling pathways and upregulates pro-inflammatory genes to reduce cancer cell viability and promote apoptosis (Caruana et al., 2017) |
Nelfinavir,1,10-phenanthroline |
Liposarcoma |
Upregulates the precursors SREBP1 and ATF6 by inhibiting the cleavage of S2P, resulting in ER stress and induction of apoptosis (Guan et al., 2011) |
Prostate cancer |
Reduces the proliferation of castration-resistant prostate cancer and promotes apoptosis through the accumulation of unprocessed SREBP1 and ATF6 (Guan et al., 2012; Guan et al., 2015) |