PBRM1/SMARCA2,4-ligand-1

PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a Ligand for Target Protein for PROTAC that binds to PBRM1, SMARCA2, and SMARCA4. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410) [1][2].

Product Specifications

CAS Number

[1997321-76-2]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Ligands for Target Protein for PROTAC

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

NC1=C(C=C(N=N1)C2=C(C=CC=C2)O)C3=CC=CC=C3

Molecular Formula

C16H13N3O

Molecular Weight

263.29

References & Citations

[1]Taylor, A. M., et al., (2022) . GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. Journal of medicinal chemistry, 65 (16), 11177–11186.|[2]Tongchen He, et al. Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer. bioRxiv [Preprint]. 2024 Mar 2:2024.02.29.582768.