Emopamil Binding Protein Inhibitor

TASIN-30 is a selective EBP inhibitor with an EC₅₀ of 0.097 μM. TASIN-30 blocks the production of 7-dehydrocholesterol (7-DHC) and downstream cholesterol biosynthesis processes. TASIN-30 depletes downstream sterols, disrupts the integrity of lipid rafts in tumor cells, accelerates intracellular cholesterol consumption, and inhibits tumor cell proliferation. TASIN-30 induces ferroptosis and apoptosis by reducing 7-DHC levels and increasing phospholipid peroxidation. TASIN-30 achieves tumor suppression in nude mice with osteosarcoma. TASIN-30 can be used in cancer-related research such as colorectal cancer and osteosarcoma.

EBP-IN-1 is an orally active, blood-brain barrier-permeable inhibitor of emopamil binding protein (EBP). EBP-IN-1 has an IC₅₀ of 8.2 μM against human ERG potassium channels (in CHO background). By inhibiting the sterol isomerase activity of EBP, EBP-IN-1 causes the accumulation of Zymostenol (HY-113345), and exhibits strong target binding in the brain after repeated administration in rodents. EBP-IN-1 also promotes oligodendrocyte formation in human cortical organoids and can be used in research related to multiple sclerosis.

DSP-0390 is an orally effective inhibitor of Emopamil-binding protein (EBP). DSP-0390 blocks the cholesterol de novo synthesis pathway in tumor cells by inhibiting EBP, and demonstrates significant anti-tumor activity in an orthotopic xenograft model of glioblastoma (GBM). DSP-0390 can be used for the study of recurrent high-grade gliomas.