Catalog No.: PC-72171Not For Human Use, Lab Use Only.
K-975 (K975, YAP1-TEAD inhibitor K975) is a potent, specific inhibitor of YAP1/TAZ-TEAD signaling, inhibits YAP1/TAZ-TEAD protein-protein interaction, a pan-TEAD inhibitor binds to Cys359 of TEAD1-YBD.
K-975 (K975, YAP1-TEAD inhibitor K975) is a potent, specific inhibitor of YAP1/TAZ-TEAD signaling, inhibits YAP1/TAZ-TEAD protein-protein interaction, a pan-TEAD inhibitor binds to Cys359 of TEAD1-YBD.
K-975 showed an inhibitory activity towards TEAD1-YAP1 PPI and TEAD4-YAP1 PPI in cells using a Halo-tag pull-down assay. Furthermore, K-975 inhibited the palmitoylation of TEAD1-YBD.
K-975 inhibits yes-associated protein 1 (YAP1)-transcriptional enhanced associate domain (TEAD) signaling by the same mechanism as YAP1 siRNA and TEADs siRNA.
K-975 decreased the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increased the expression of FBXO32 mRNA with 24-h treatment in NCI-H226 cells.
K-975 exerts a stronger inhibitory activity towards neurofibromin 2 (NF2)-non-expressing mesothelioma cell lines.
K-975 exerts an anti-tumor effect and significant survival benefit in human mesothelioma xenograft mice.
K-975 exhibits a synergistic effect with a CDK4/6 inhibitor palbociclib in s.c. transplant mouse models of human mesothelioma.
Physicochemical Properties
M.Wt
287.743
Formula
C16H14ClNO2
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-(3-(4-chlorophenoxy)-4-methylphenyl)acrylamide
References
1. Kaneda A, et al. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415.
