PROTAC TEAD1/IAP degrader-2
PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research.
(Pink: TEAD1 ligand (HY-181538); Blue: IAP ligand (HY-181531); Black: linker (HY-W803227)).
For research use only. We do not sell to patients.
- Formula: C48H44F3N11O3S
- Molecular Weight:912.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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TEAD1 170 nM (DC50) |
cIAP |
PROTAC TEAD1/IAP degrader-2 (Compound A531) (1 nM-10000 nM; 144 h) inhibits the proliferation of Hippo pathway-dependent mesothelioma cells (ZL55, NCI-H226, NCI-H2052) as well as Hippo pathway-independent NCI-H520 cells; among these, it exhibits the strongest activity in NCI-H226 cells (IC50 = 310 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 912.00
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Formula C48H44F3N11O3S
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SMILES
O=C(C1=CC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2N=C1)NCC4=NC(N5CCN(C(CN6N=C(C)C(C7=CC=C(NC([C@@H](NC)C)=O)N=C7C#CC8=CN=CS8)=C6C)=O)CC5)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)