SWTX-143 | TEAD inhibitor | Probechem Biochemicals

Chemical Structure : SWTX-143

SWTX-143 (SWTX143)

Catalog No.: PC-21317Not For Human Use, Lab Use Only.

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

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Biological Activity

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

SWTX-143 potently represses luciferase expression from the TEAD reporter (IC50=12 nmol/L) while not affecting the viability of HEK293 cells.

SWTX-143 is sufficient to evoke a long-lasting transcriptional impact.

SWTX-143 inhibits the proliferation of Hippo pathway-mutant cancer cell lines with IC50 of 5-207 nM against three distinct desothelioma cancer cell lines that are characterized by and depend on loss-of-function alterations in NF2 (Mero-14, NCI-H226, and CI-H2052) and one that is deficient in ATS1 and LATS2 (MSTO-211H).

SWTX-143 only modestly impacts the proliferation of the NCI-H28 and NCI-H2452 mesothelioma, HeLa, SiHa, and CaSki cancer cell lines which lack genetic alterations in known Hippo pathway components (Hippo-WT).

SWTX-143 (10, 25, and 50 mg/kg) causes regression of NF2-deficient human mesothelioma xenografts.

SWTX-143 also selectively impairs the growth of NF2-mutant kidney cancer cell lines, blocks Hippo pathway transcriptional output and causes tumor regression in preclinical mesothelioma models.

Physicochemical Properties

M.Wt	361.37
Formula	C19H18F3N3O
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	N-[5-Amino-1,2,3,4-tetrahydro-1-[4-(trifluoromethyl)phenyl]-3-quinolinyl]-2-propenamide

References

1. Hanne Hillen, et al. Mol Cancer Ther. 2023 Sep 23. doi: 10.1158/1535-7163.MCT-22-0681.

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SWTX-143 (SWTX143)

Biological Activity

Physicochemical Properties

References

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