BPI-460372 is a potent and selective inhibitor of the TEAD transcription factors TEAD1, TEAD3, and TEAD4, which are downstream effectors in the Hippo signaling pathway and are implicated in various cancers. In biochemical assays, BPI-460372 demonstrates high-affinity binding to TEAD1–4 through covalent modification of a conserved cysteine residue in the TEAD central pocket, thereby disrupting its interaction with the transcriptional coactivator YAP. The compound exhibits low nanomolar inhibitory activity, with IC₅₀ values reported in the range of 10–50 nM against TEAD-driven transcriptional activity in cell-based luciferase reporter assays. In cancer cell lines reliant on YAP/TEAD signaling, such as mesothelioma and certain squamous cell carcinomas, BPI-460372 suppresses cell proliferation and TEAD target gene expression (e.g., CTGF, CYR61), showing EC₅₀ values typically between 50–200 nM.
MedKoo Cat#: 128463
Name: BPI-460372
CAS#: 2762619-63-4
Chemical Formula: C18H13F4N5O2
Exact Mass: 407.1005
Molecular Weight: 407.33
Elemental Analysis: C, 53.08; H, 3.22; F, 18.66; N, 17.19; O, 7.86
The following data is based on the product molecular weight 407.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
