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BI-78D3
- Development stage
- Preclinical
- Lead developer
- Sanford Burnham Prebys Medical Discovery Institute
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
BI-78D3 is a small molecule, substrate-competitive inhibitor of c-Jun N-terminal kinase (JNK) that targets the JNK-interacting protein-1 (JIP1) scaffolding binding site, also known as the D-recruitment site (DRS). Developed by the Sanford Burnham Prebys Medical Discovery Institute, BI-78D3 prevents the interaction between JNK and its scaffolding protein JIP1, thereby inhibiting JNK phosphorylation and downstream signaling. It has been widely used as a chemical probe in preclinical research to study JNK-dependent pathways in various conditions, including type 2 diabetes, inflammatory diseases, and oncology. Additionally, BI-78D3 has been shown to covalently bind and inhibit extracellular signal-regulated kinase 2 (ERK2) and disrupt the NPAS3-ARNT transcription factor complex.
- Other names
- JNK Inhibitor X
02
Targets
JNK (Mitogen-activated protein kinase kinase kinase family)MAPK14 (p38 mitogen-activated protein kinase alpha)
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