Name: PROTAC ERRalpha Degrader-2
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

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

(E)-N-[5-[[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]pentyl]-3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyanoprop-2-enamide

InChI Key

BCMRBUQELZGQDK-ZAZFVFGXSA-N

InChI

InChI=1S/C57H55Cl2F6N7O8/c1-34(2)80-47-29-43(77-3)19-20-44(47)53-69-51(36-10-15-41(58)16-11-36)52(37-12-17-42(59)18-13-37)72(53)55(76)71-25-24-70(50(74)32-71)31-49(73)67-22-6-5-7-23-68-54(75)39(30-66)26-35-8-21-46(48(27-35)78-4)79-33-38-9-14-40(56(60,61)62)28-45(38)57(63,64)65/h8-21,26-29,34,51-52H,5-7,22-25,31-33H2,1-4H3,(H,67,73)(H,68,75)/b39-26+/t51-,52+/m1/s1

SMILES

CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)NCCCCCNC(=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-2 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

• PROTAC-Mediated Degradation: PROTAC ERRalpha Degrader-2 offers a robust approach to selectively degrade estrogen-related receptor alpha (ERRα) in cellular models. By harnessing the ubiquitin-proteasome system, this degrader facilitates the study of ERRα's role in metabolic regulation and its potential as a therapeutic target in metabolic disorders.

• Targeted Protein Degradation in Cancer Research: Utilizing PROTAC ERRalpha Degrader-2 enables researchers to explore the therapeutic implications of ERRα degradation in cancer models. This tool aids in dissecting the molecular pathways influenced by ERRα and its contribution to tumorigenesis, providing insights into novel anti-cancer strategies.

• Functional Genomics Studies: With PROTAC ERRalpha Degrader-2, scientists can perform precise functional genomics analyses by degrading ERRα. This approach helps elucidate the transcriptional networks governed by ERRα, advancing our understanding of its regulatory mechanisms in various physiological and pathological contexts.

• Drug Discovery and Development: PROTAC ERRalpha Degrader-2 serves as a valuable asset in drug discovery pipelines focused on targeted protein degradation. It facilitates the identification and validation of ERRα as a drug target, accelerating the development of innovative therapeutic agents targeting this receptor.

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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