2. PROTAC Stem Cell/Wnt
  3. PROTACs YAP
  4. PROTAC TEAD degrader-1

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)).

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PROTAC TEAD degrader-1

PROTAC TEAD degrader-1 Estructura química

No. CAS : 3061498-57-2

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PROTAC TEAD degrader-1 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Ver todos los productos específicos de isoformas YAP:

Ver todas las isoformas
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • Actividad biológica

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Descripciòn

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[1]. (Pink: TEAD2 ligand (HY-158400); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W008474)).

IC50 & Target[1]

TEAD2

32.7 nM (DC50)

Cellular Effect
Cell Line Type Value Description References
NCI-H226 IC50
0.21 μM
Compound: 27
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
[PMID: 38746898]
NCI-H2452 IC50
> 10 μM
Compound: 27
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
[PMID: 38746898]
In Vitro

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.

PROTAC TEAD degrader-1 Related Antibodies

Real Time qPCR[1]

Cell Line: NF2-deficient NCI-H226 cells
Concentration: 0.5 and 1 μM
Incubation Time: 8 h
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.
Peso molecular

822.83

Fòrmula

C44H41F3N6O7
No. CAS
Appearance

Solid

Color

Light yellow to yellow

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2153 mL 6.0766 mL 12.1532 mL
5 mM --- --- ---
View the 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.

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Pureza y Documentación
Referencias

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
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PROTAC TEAD degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC TEAD degrader-13061498-57-2PROTAC TEAD degrader1PROTAC TEAD degrader 1PROTACsYAPYes-associated proteinproteasome systemNCI-H2452 cellsTEAD2CTGFNF2-deficient cancerCRBNCYR61YAP target genes293T cellsNCI-H226 cellsInhibitorinhibitorinhibit

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Nombre del producto:
PROTAC TEAD degrader-1
Cat. No.:
HY-158342
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