Chemical Structure : BPI-460372
货号: 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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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.
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外观性状 | Solid | |
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Solubility |
10 mM in DMSO |
1. Xiaohong Han, et al. Cancer Res (2024) 84 (6_Supplement): 7575.
2. Hongling Shen, et al. Cancer Res (2023) 83 (7_Supplement): 501.
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