TEAD degrader-1
TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC50 of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 3103984-17-1
- Formula: C36H38ClF2N3O6
- Molecular Weight:682.15
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All YAP Isoforms
More
Biological Activity
|
TEAD 3.1 nM (IC50) |
TEAD degrader-1 (compound 15) potently inhibits the TEAD1-YAP1 protein-protein interaction with an IC50 of 3.1 nM in a cell-free biochemical assay[1].
TEAD degrader-1 potently and rapidly degrades TEAD in NCI-H226 mesothelioma cells, with a DC50 of 1.9 nM (6 h, 97% Dmax) and 1.0 nM (24 h, 98% Dmax), and sustained deep degradation for up to 72 hours[1].
TEAD degrader-1 (24 h) potently degrades TEAD in MSTO-211H mesothelioma cells, achieving > 72% maximal degradation with a DC50 < 80 nM after 24 hours[1].
TEAD degrader-1 (24 h) potently inhibits TEAD target gene (CCN1, CCN2) expression in MSTO-211H mesothelioma cells, with > 90% maximal inhibition and an IC50 < 2 nM after 24 hours[1].
TEAD degrader-1 (120 h) potently inhibits the viability of Hippo pathway-dysregulated MSTO-211H mesothelioma cells, achieving >95% maximal growth inhibition after 120 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 3103984-17-1
-
Molecular Weight 682.15
-
Formula C36H38ClF2N3O6
-
SMILES
O=C(N)C1=[C@]([C@]2=C(Cl)C(F)=CC3=C2[C@H](C)[C@](C4=CC=CC=C4)(CN[C@@H]5CC[C@@H](C(N6CC(C=O)OCC6)=O)CC5)O3)C(F)=C(OC)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
Powered by Bioz