Name: PROTAC ERRalpha Degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

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Stock

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$--

In stock

Solubility

10 mM in DMSO

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Synonyms

PROTAC ERRalpha Degrader 1; (E)-N-[2-[[2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetyl]amino]ethyl]-3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyanoprop-2-enamide

InChI Key

ZVQCWVLBPYOZNC-XNCCLBLBSA-N

InChI

InChI=1S/C54H49Cl2F6N7O8/c1-31(2)77-44-26-40(74-3)16-17-41(44)50-66-48(33-7-12-38(55)13-8-33)49(34-9-14-39(56)15-10-34)69(50)52(73)68-22-21-67(47(71)29-68)28-46(70)64-19-20-65-51(72)36(27-63)23-32-5-18-43(45(24-32)75-4)76-30-35-6-11-37(53(57,58)59)25-42(35)54(60,61)62/h5-18,23-26,31,48-49H,19-22,28-30H2,1-4H3,(H,64,70)(H,65,72)/b36-23+/t48-,49+/m1/s1

SMILES

CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)NCCNC(=O)C(=CC4=CC(=C(C=C4)OCC5=C(C=C(C=C5)C(F)(F)F)C(F)(F)F)OC)C#N)C6=CC=C(C=C6)Cl)C7=CC=C(C=C7)Cl

Mechanism

Target: Targets estrogen-related receptor alpha (ERRα) for experimental targeted protein degradation studies.

Binding Site: Binds the ERRα ligand-binding domain and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: PROTAC ERRalpha Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward estrogen-related receptor alpha (ERRα). The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• Targeted Degradation of ERRalpha: This PROTAC ERRalpha Degrader-1 is designed for the precise degradation of Estrogen-Related Receptor alpha (ERRalpha), a pivotal transcription factor in energy metabolism and cancer. Researchers can utilize this degrader to investigate ERRalpha's role in cellular processes by observing the phenotypic consequences of its targeted degradation.

• PROTAC-Based Metabolic Studies: By employing PROTAC ERRalpha Degrader-1, scientists can explore the metabolic pathways influenced by ERRalpha. This tool facilitates the dissection of ERRalpha's involvement in metabolic regulation, providing insights into its potential as a therapeutic target in metabolic disorders.

• Functional Protein Knockdown: The PROTAC ERRalpha Degrader-1 enables researchers to achieve functional knockdown of ERRalpha in cellular models. This application is crucial for studying protein function and validating ERRalpha as a target for therapeutic intervention in diseases where its activity is dysregulated.

• Investigation of Cancer Pathways: Utilizing the PROTAC ERRalpha Degrader-1 allows for the exploration of ERRalpha's contribution to oncogenic pathways. This application aids in understanding how ERRalpha degradation affects tumor growth and survival, offering a valuable approach for cancer research.

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂