PROTAC MDM2 Degrader-2

 CAS No.: 2249944-99-6  Cat No.: BP-400064 4.5  

PROTAC MDM2 Degrader-2 is a specialized chemical agent designed for targeted protein degradation, specifically targeting the MDM2 protein, a key regulator in the p53 tumor suppressor pathway. This degrader operates by binding to the MDM2 protein at its designated binding site, facilitating its ubiquitination and subsequent proteasomal degradation. The molecular architecture of PROTAC MDM2 Degrader-2 is engineered to include a ligand for MDM2, a linker, and an E3 ligase recruiting moiety, which together form a bifunctional molecule. Within the PROTAC framework, this degrader plays a critical role by bridging the target protein MDM2 with an E3 ubiquitin ligase, thereby promoting selective degradation. The primary mechanism involves the recruitment of the ubiquitin-proteasome system to MDM2, leading to its efficient breakdown and the modulation of downstream signaling pathways. This product is invaluable in research focused on cancer biology and therapeutic development, offering a potent tool for elucidating the roles of MDM2 in oncogenesis and exploring novel avenues for targeted cancer therapies.

PROTAC MDM2 Degrader-2

Structure of 2249944-99-6

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Category
PROTAC
Molecular Formula
C70H76Cl4N10O12
Molecular Weight
1391.22

* 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 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]-N-[2-[2-[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]ethoxy]ethoxy]ethyl]acetamide
InChI Key
WZLSSHVSGKCEKQ-AKOOKZATSA-N
InChI
InChI=1S/C70H76Cl4N10O12/c1-43(2)95-57-37-53(91-5)23-25-55(57)67-77-63(45-7-15-49(71)16-8-45)65(47-11-19-51(73)20-12-47)83(67)69(89)81-31-29-79(61(87)41-81)39-59(85)75-27-33-93-35-36-94-34-28-76-60(86)40-80-30-32-82(42-62(80)88)70(90)84-66(48-13-21-52(74)22-14-48)64(46-9-17-50(72)18-10-46)78-68(84)56-26-24-54(92-6)38-58(56)96-44(3)4/h7-26,37-38,43-44,63-66H,27-36,39-42H2,1-6H3,(H,75,85)(H,76,86)/t63-,64-,65+,66+/m1/s1
SMILES
CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCN(C(=O)C3)CC(=O)NCCOCCOCCNC(=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-2 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 facilitates the targeted degradation of MDM2, a key regulator in the p53 tumor suppressor pathway. By employing a bifunctional molecule, it recruits E3 ligases to ubiquitinate and degrade MDM2, providing a powerful tool for studying MDM2's role in cancer biology and therapeutic resistance mechanisms.

• Targeted Protein Degradation in Oncology: PROTAC MDM2 Degrader-2 allows researchers to explore novel cancer treatment strategies by effectively reducing MDM2 levels. This application aids in elucidating the impact of MDM2 degradation on tumor suppression and offers insights into the development of new therapeutic approaches targeting oncogenic pathways.

• Investigating Protein-Protein Interactions: Utilizing PROTAC technology, this degrader enables the study of protein-protein interactions involving MDM2. By selectively degrading MDM2, researchers can dissect its interaction networks and downstream effects, advancing the understanding of cellular processes and signaling pathways influenced by MDM2.

• Modulating Cellular Pathways: The targeted degradation of MDM2 using this PROTAC compound offers a strategic approach to modulate cellular pathways. Researchers can investigate the consequences of MDM2 depletion on cell cycle regulation, apoptosis, and DNA damage response, providing insights into potential intervention points for therapeutic development.

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L

* 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

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g

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