Name: PROTAC BET degrader-2
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Solubility

H2O : < 0.1 mg/mL (insoluble); DMSO : 50 mg/mL (64.86 mM; Need ultrasonic)

Storage

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping

Room temperature in continental US; may vary elsewhere

Synonyms

PROTAC BET degrader 2; 4-[(5-cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-[3-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]propyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

InChI Key

LKCUEUQTTCOYPW-UHFFFAOYSA-N

InChI

InChI=1S/C41H42N10O6/c1-5-51-32(18-28(48-51)23-11-12-23)44-37-35-25-17-31(56-4)26(34-20(2)49-57-21(34)3)16-29(25)43-36(35)46-38(47-37)40(54)42-15-7-9-22-8-6-10-24-27(22)19-50(41(24)55)30-13-14-33(52)45-39(30)53/h6,8,10,16-18,23,30H,5,7,9,11-15,19H2,1-4H3,(H,42,54)(H,45,52,53)(H2,43,44,46,47)

SMILES

CCN1C(=CC(=N1)C2CC2)NC3=NC(=NC4=C3C5=CC(=C(C=C5N4)C6=C(ON=C6C)C)OC)C(=O)NCCCC7=C8CN(C(=O)C8=CC=C7)C9CCC(=O)NC9=O

Mechanism

Target: Targets BET bromodomain proteins, especially BRD4, BRD3, and BRD2 for experimental targeted protein degradation studies.

Binding Site: Binds the BET bromodomain acetyl-lysine pocket and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: PROTAC BET degrader-2 is designed for use in PROTAC or targeted protein degradation experiments directed toward BET bromodomain proteins, especially BRD4, BRD3, and BRD2. 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 BET Degradation: PROTAC BET degrader-2 is designed to selectively target and degrade BET proteins, which are key regulators of gene expression. This application is crucial for understanding BET protein roles in epigenetic regulation and their potential implications in various diseases, providing a powerful tool for mechanistic studies in cellular models.

• Targeted Protein Degradation in Oncology: By utilizing PROTAC BET degrader-2, researchers can explore the therapeutic potential of degrading BET proteins in cancer models. This approach allows for the dissection of BET protein functions in tumorigenesis and the identification of novel therapeutic strategies, enhancing our understanding of cancer biology.

• Epigenetic Modulation via PROTACs: The application of PROTAC BET degrader-2 facilitates the study of epigenetic changes through targeted degradation of BET proteins. This tool aids in deciphering the complex networks of gene regulation and chromatin remodeling, offering insights into the molecular mechanisms underlying various epigenetic disorders.

• Mechanistic Studies in Drug Resistance: Employing PROTAC BET degrader-2 enables the investigation of resistance mechanisms in cells by degrading BET proteins involved in drug response pathways. This application is vital for developing strategies to overcome resistance and improve the efficacy of existing therapeutic agents.

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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