PROTAC MDM2 Degrader-3

 CAS No.: 2249750-23-8  Cat No.: BP-400002 4.5  

PROTAC MDM2 Degrader-3 is a specialized small molecule designed to selectively target the MDM2 protein, a key regulator in the ubiquitin-proteasome pathway. This degrader binds specifically to the MDM2 protein at its defined binding site, facilitating its interaction with an E3 ubiquitin ligase. The molecular architecture of PROTAC MDM2 Degrader-3 includes a ligand for MDM2, a linker, and a ligand for the E3 ligase, orchestrating the proximity-induced ubiquitination of MDM2. This process results in the proteasomal degradation of MDM2, thereby modulating p53 activity and influencing cell cycle regulation. In the context of PROTAC design, PROTAC MDM2 Degrader-3 serves as a vital tool for elucidating the mechanisms of targeted protein degradation. It is instrumental in research aimed at understanding the therapeutic potential of degrading oncogenic proteins. Its application extends to studies focused on the development of novel cancer therapies, offering a robust platform for investigating the dynamics of protein-protein interactions and degradation pathways in cellular models.

PROTAC MDM2 Degrader-3

Structure of 2249750-23-8

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PROTAC
Molecular Formula
C72H78Cl4N8O15
Molecular Weight
1437.25

* For research and manufacturing use only. Not for human or clinical use.

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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 MDM2 Degrader 3; 2-[2-[2-[2-[2-[4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetyl]oxyethoxy]ethoxy]ethoxy]ethyl 2-[4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetate
InChI Key
KECKJSNYFPFODX-PINBWVOXSA-N
InChI
InChI=1S/C72H78Cl4N8O15/c1-45(2)98-59-39-55(91-5)23-25-57(59)69-77-65(47-7-15-51(73)16-8-47)67(49-11-19-53(75)20-12-49)83(69)71(89)81-29-27-79(61(85)41-81)43-63(87)96-37-35-94-33-31-93-32-34-95-36-38-97-64(88)44-80-28-30-82(42-62(80)86)72(90)84-68(50-13-21-54(76)22-14-50)66(48-9-17-52(74)18-10-48)78-70(84)58-26-24-56(92-6)40-60(58)99-46(3)4/h7-26,39-40,45-46,65-68H,27-38,41-44H2,1-6H3/t65-,66-,67+,68+/m0/s1
SMILES
CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)OCCOCCOCCOCCOC(=O)CN4CCN(CC4=O)C(=O)N5C(C(N=C5C6=C(C=C(C=C6)OC)OC(C)C)C7=CC=C(C=C7)Cl)C8=CC=C(C=C8)Cl)C9=CC=C(C=C9)Cl)C1=CC=C(C=C1)Cl
Mechanism

Target: Targets MDM2 E3 ligase protein for experimental targeted protein degradation studies.

Binding Site: Binds the MDM2 p53-binding cleft and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: PROTAC MDM2 Degrader-3 is designed for use in PROTAC or targeted protein degradation experiments directed toward MDM2 E3 ligase protein. 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 MDM2 Degradation: PROTAC MDM2 Degrader-3 is utilized in research to selectively degrade the MDM2 oncoprotein. By facilitating ubiquitination and subsequent proteasomal degradation, this compound helps dissect the role of MDM2 in cancer biology, offering insights into tumorigenesis and potential therapeutic strategies targeting the MDM2-p53 axis.

• Targeted Protein Degradation in Oncology: This PROTAC tool enables researchers to explore the degradation of MDM2 in cancer cells, providing a powerful approach to study the modulation of oncogenic pathways. It aids in understanding how targeted degradation can influence cell cycle regulation and apoptosis in malignancies.

• Mechanistic Studies of PROTACs: PROTAC MDM2 Degrader-3 serves as a model compound for investigating the mechanistic aspects of PROTAC technology. Researchers can use it to examine the efficiency of E3 ligase recruitment and target protein ubiquitination, contributing to the broader understanding of PROTAC design and function.

• Advancing Drug Discovery: By employing PROTAC MDM2 Degrader-3, scientists can evaluate the potential of targeted protein degradation in drug discovery pipelines. This application supports the development of novel therapeutic agents that exploit the ubiquitin-proteasome system for selective protein elimination, broadening the horizons of precision medicine.

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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

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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