1. PROTAC
  2. Ligand for E3 Ligase
  3. AR antagonist 1

AR antagonist 1 

Cat. No.: HY-130845
Handling Instructions

AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

For research use only. We do not sell to patients.

AR antagonist 1 Chemical Structure

AR antagonist 1 Chemical Structure

CAS No. : 1818885-54-9

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Description

AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

IC50 & Target

IC50: androgen receptor[1]

In Vitro

AR antagonist 1 (compound 29) is the ligand for target ligase of ARD-266. ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader.
AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex, it can be successfully employed for the design of highly potent and efficient PROTAC degraders.
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein.
PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

Molecular Weight

278.78

Formula

C₁₅H₁₉ClN₂O

CAS No.

1818885-54-9

SMILES

N#CC1=CC=C(O[[email protected]]2C(C)(C)[[email protected]](N)C2(C)C)C=C1Cl

Shipping

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AR antagonist 1AR antagonist1AR antagonist-1Ligand for E3 LigaseE3 ligase-recruiting MoietyPROTACLinkertumorcancerLNCaPVCaPInhibitorinhibitorinhibit

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AR antagonist 1
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HY-130845
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