An inhibitor of the YAP/TAZ-TEAD1 and YAP/TAZ-TEAD4 protein-protein interactions
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VT107

Item No. 46238

Technical Information
Formal Name
N-[(1S)-1-(6-amino-2-pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide
CAS Number
2417718-63-7
Molecular Formula
C25H20F3N3O
Formula Weight
Purity
≥98%
A solid
SMILES
C[C@@H](C1=CC=CC(N)=N1)NC(C2=CC3=C(C=C2)C(C4=CC=C(C=C4)C(F)(F)F)=CC=C3)=O
InChi Code
InChI=1S/C25H20F3N3O/c1-15(22-6-3-7-23(29)31-22)30-24(32)18-10-13-21-17(14-18)4-2-5-20(21)16-8-11-19(12-9-16)25(26,27)28/h2-15H,1H3,(H2,29,31)(H,30,32)/t15-/m0/s1
InChi Key
OBEXKSHQMHIUFP-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VT107 is an inhibitor of the protein-protein interaction between YAP/TAZ and TEAD1 or TEAD4.1 It inhibits autopalmitoylation of TEAD1-4 in HEK293 cells expressing the human transcription factors when used at 3 µM and inhibits YAP/TAZ-TEAD transcriptional activity in a cell-based reporter assay (IC50 = 4.93 nM). VT107 inhibits the growth of NF2-deficient NCI-H2052 and NCI-H2373 mesothelioma and NCI H226 lung cancer cells (IC50s = 20.4, 9.35, and 8.67 nM, respectively) but not wild-type NF2-expressing NCI H28, NCI 2452, or MSTO-211H cells (IC50s = 2,790, >3,000, and >3,000 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tang, T.T., Konradi, A.W., Feng, Y., et al. Small molecule inhibitors of TEAD auto-palmitoylation selectively inhibit proliferation and tumor growth of NF2-deficient mesothelioma. Mol. Cancer Ther. 20(6), 986-998 (2021).