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BPI-460372

Chemical Structure : BPI-460372

CAS No.:

BPI-460372

Catalog No.: PC-23994Not For Human Use, Lab Use Only.

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.
BPI-460372 significantly inhibits the expression of a TEAD-responsive element reporter, as well as the mRNA of downstream target genes such as CTGF and CYR61 in NF2-deficient cells.
BPI-460372 strongly inhibited the proliferation of tumor cells harboring Hippo pathway aberrations.
BPI-460372 significantly suppressed tumor growth in NF2-deficient or LATS1/2 mutation xenograft models.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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