PROTAC TEAD degrader-2
PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma.
(Pink: TEAD1 ligand (HY-186022); Blue: Cereblon ligand (HY-122725); Black: linker (HY-76199)).
For research use only. We do not sell to patients.
- CAS No.: 2918762-17-9
- Formula: C49H52ClF2N5O7
- Molecular Weight:896.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
TEAD1 0.6 nM (DC50) |
YAP/TAZ-TEAD 1.8 nM (IC50) |
In Vitro
Chemical Information
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CAS No. 2918762-17-9
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Molecular Weight 896.42
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Formula C49H52ClF2N5O7
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SMILES
O=C(C1=[C@@]([C@@]2=C3[C@H](C)[C@](C4=CC=CC=C4)(CN[C@@H]5CC[C@H](CC5)C(NCCCCCC(C=CC=C67)=C7CN(C8C(NC(CC8)=O)=O)C6=O)=O)OC3=CC(F)=C2Cl)C(F)=C(OC)C=C1)N
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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.
Protocols
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- PROTAC TEAD degrader-2
- 2918762-17-9
- PROTAC TEAD degrader2
- PROTAC TEAD degrader 2
- PROTACs
- YAP
- YAP/TAZ-TEAD inhibitor
- PROTAC
- TEAD degradation
- protein-protein interaction
- cancer therapy
- Hippo pathway
- ubiquitin-proteasome system
- biochemical assay
- cellular proliferation
- luciferase reporter assay
- Inhibitor
- inhibitor
- inhibit