PROTAC TEAD degrader-1
Based on 1 Customer Validation
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer.
(Pink: TEAD2 ligand (HY-158400); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W008474)).
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 3061498-57-2
- Formula: C44H41F3N6O7
- Molecular Weight:822.83
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TEAD2 32.7 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H226 | IC50 |
0.21 μM
Compound: 27
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Antiproliferative activity against human NCI-H226 cells incubated for 120 hrs by Celltiter-glo luminescent assay
Antiproliferative activity against human NCI-H226 cells incubated for 120 hrs by Celltiter-glo luminescent assay
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[PMID: 38746898] |
| NCI-H2452 | IC50 |
>10 μM
Compound: 27
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Antiproliferative activity against human NCI-H2452 cells incubated for 120 hrs by Celltiter-glo luminescent assay
Antiproliferative activity against human NCI-H2452 cells incubated for 120 hrs by Celltiter-glo luminescent assay
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[PMID: 38746898] |
PROTAC TEAD degrader-1 (Compound 27) (9.75-10000 nM; 24 h) acts as a selective degrader of TEAD2 in Flag-TEAD transfected 293T cells, with a DC50 of 54.1 nM against Flag-TEAD2. It exhibits extremely low activity against Flag-TEAD1 and no activity against Flag-TEAD3 or Flag-TEAD4[1].
PROTAC TEAD degrader-1 (5 d) potently inhibits the proliferation of NF2-deficient NCI-H226 cells with an IC50 of 0.21 μM, while exhibits significantly lower activity against NF2-wildtype NCI-H2452 cells[1].
PROTAC TEAD degrader-1 (0.5-1 μM; 8 h) downregulates the expression of YAP target genes in a concentration-dependent manner and upregulates FBXO32 expression in NCI-H226 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NF2-deficient NCI-H226 cells
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Concentration:0.5 and 1 μM
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Incubation Time:8 h
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Result:Concentration-dependently decreased the mRNA expression levels of YAP target genes CYR61, IGFBP3, AMOTL2, CTGF, and NPPB.
Increased the mRNA expression level of the FBXO32 gene.
Chemical Information
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CAS No. 3061498-57-2
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Appearance Solid
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Molecular Weight 822.83
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Formula C44H41F3N6O7
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Color Light yellow to yellow
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SMILES
O=C(N[C@H](C1=NC(NCCOCCOCCNC2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)=CC=C1)C)C5=CC=C6C(C7=CC=C(C(F)(F)F)C=C7)=CC=CC6=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 2 mg/mL (2.43 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2153 mL | 6.0766 mL | 12.1532 mL | 30.3829 mL |
PROTAC TEAD degrader-1 Related Classifications
HY-158342 Related Classifications
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