Name: PROTAC MDM2 Degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

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 MDM2 Degrader 1; 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]-N-[3-[2-[2-[3-[[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]propoxy]ethoxy]ethoxy]propyl]acetamide

InChI Key

AQFZQNOXRSZHMG-PQMVWXROSA-N

InChI

InChI=1S/C74H84Cl4N10O13/c1-47(2)100-61-41-57(95-5)25-27-59(61)71-81-67(49-9-17-53(75)18-10-49)69(51-13-21-55(77)22-14-51)87(71)73(93)85-33-31-83(65(91)45-85)43-63(89)79-29-7-35-97-37-39-99-40-38-98-36-8-30-80-64(90)44-84-32-34-86(46-66(84)92)74(94)88-70(52-15-23-56(78)24-16-52)68(50-11-19-54(76)20-12-50)82-72(88)60-28-26-58(96-6)42-62(60)101-48(3)4/h9-28,41-42,47-48,67-70H,7-8,29-40,43-46H2,1-6H3,(H,79,89)(H,80,90)/t67-,68-,69+,70+/m1/s1

SMILES

CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)NCCCOCCOCCOCCCNC(=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-1 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: This product is designed for the targeted degradation of the MDM2 protein, a crucial regulator of the p53 tumor suppressor pathway. By promoting the ubiquitination and subsequent proteasomal degradation of MDM2, researchers can explore the restoration of p53 activity, providing insights into cancer biology and potential therapeutic strategies.

• Targeted Protein Degradation in Oncology: Utilize PROTAC MDM2 Degrader-1 to investigate the role of MDM2 in various cancer models. This degrader facilitates the study of MDM2's involvement in tumor progression and resistance mechanisms, allowing for the identification of novel intervention points within oncogenic pathways.

• Mechanistic Studies of MDM2-p53 Interaction: Employ this PROTAC to dissect the molecular interactions between MDM2 and p53. By degrading MDM2, researchers can delineate the downstream effects on p53 stabilization and activity, enhancing the understanding of cell cycle regulation and apoptosis in cancer research.

• Drug Resistance Research: PROTAC MDM2 Degrader-1 serves as a powerful tool to study mechanisms of drug resistance associated with MDM2 overexpression. By selectively degrading MDM2, researchers can evaluate the effects on treatment efficacy and explore combination therapies to overcome resistance in cancer cells.

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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