ARD-1676

 CAS No.: 2632305-36-1  Cat No.: BP-400198 4.5  

ARD-1676 is a cereblon-recruiting PROTAC degrader targeting the androgen receptor. Published work describes it as a highly potent androgen receptor degrader designed from a new class of AR ligands and a novel cereblon ligand. The AR-recognition module engages the receptor target, while the cereblon ligand recruits CRL4-cereblon ubiquitination machinery through the opposite end of the molecule. Mechanistically, ARD-1676 induces AR ubiquitination and proteasome-dependent degradation, enabling suppression of androgen receptor protein functions rather than receptor occupancy alone. It is valuable for studying androgen receptor signaling, nuclear receptor degrader design, ligand-binding-domain-directed target removal, resistance-associated AR biology, transcriptional consequences of AR depletion, and comparison of cereblon-recruiting AR degraders with VHL-based or antagonist-only approaches in prostate cancer research models.

ARD-1676

Structure of 2632305-36-1

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Category
PROTAC
Molecular Formula
C44H46ClN7O5
Molecular Weight
788.33
Appearance
White to light yellow solid

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

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Appearance
White to light yellow solid
Storage
Store at 4 °C
IUPACName
2-chloro-4-[(3S)-8-[4-[4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-5,7-dihydropyrrolo[3,4-f]isoindol-6-yl]methyl]piperidine-1-carbonyl]phenyl]-3-methyl-2,8-diazaspiro[4.5]decan-2-yl]benzonitrile
Synonyms
ARD 1676; ARD1676; Pak8EC5gpr
InChI Key
GAXWAKXJBZHVQF-ZVENJKCTSA-N
InChI
InChI=1S/C44H46ClN7O5/c1-27-21-44(26-51(27)34-7-4-30(22-46)37(45)20-34)12-16-49(17-13-44)33-5-2-29(3-6-33)41(55)50-14-10-28(11-15-50)23-48-24-31-18-35-36(19-32(31)25-48)43(57)52(42(35)56)38-8-9-39(53)47-40(38)54/h2-7,18-20,27-28,38H,8-17,21,23-26H2,1H3,(H,47,53,54)/t27-,38?/m0/s1
SMILES
C[C@H]1CC2(CCN(CC2)C3=CC=C(C=C3)C(=O)N4CCC(CC4)CN5CC6=CC7=C(C=C6C5)C(=O)N(C7=O)C8CCC(=O)NC8=O)CN1C9=CC(=C(C=C9)C#N)Cl
Mechanism

Target: Targets androgen receptor variants, including full-length AR and AR-V7 for experimental targeted protein degradation studies.

Binding Site: Binds the AR ligand-binding or variant-associated domain and E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: ARD-1676 is designed for use in PROTAC or targeted protein degradation experiments directed toward androgen receptor variants, including full-length AR and AR-V7. 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 Oncogene Degradation: ARD-1676 is utilized in research to selectively degrade oncogenic proteins, offering a novel approach to study cancer biology. By targeting specific oncogenes for degradation, researchers can dissect their roles in tumorigenesis and explore potential therapeutic interventions.

• Targeted Degradation in Neurodegeneration: Researchers employ ARD-1676 to investigate the degradation of proteins implicated in neurodegenerative diseases. This application aids in understanding the pathophysiology of disorders like Alzheimer's and Parkinson's, potentially leading to the identification of novel therapeutic targets.

• Selective Protein Knockdown: ARD-1676 facilitates the targeted knockdown of proteins with high specificity, allowing scientists to study protein function and interaction networks. This application is crucial for elucidating the roles of difficult-to-target proteins in various cellular processes.

• PROTAC-Driven Signal Pathway Analysis: By using ARD-1676, researchers can selectively degrade key signaling proteins, providing insights into complex signaling pathways. This approach helps in mapping out signal transduction mechanisms and understanding cellular responses to environmental stimuli.

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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

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

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