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E3 ligase Ligand 1

Names

[ CAS No. ]:
1948273-03-7

[ Name ]:
E3 ligase Ligand 1

Biological Activity

[Description]:

E3 ligase Ligand 1 is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.

[Related Catalog]:

Signaling Pathways >> PROTAC >> Ligand for E3 Ligase
Research Areas >> Cancer

[Target]

Ligand for E3 Ligase[1]


[In Vitro]

E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand[1]. E3 ligase Ligand 1 is used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].

[References]

[1]. WO/2017/030814A1

[2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129


[Related Small Molecules]

TC E3 5031 | VH 298 | 2-(2,6-dioxopiperidin-3-yl)-4-hydroxyisoindoline-1,3-dione | Thalidomide fluoride | E3 ligase Ligand 1A | E3 ligase Ligand 5 | E3 ligase Ligand 6 | TNF-α-IN-1

Chemical & Physical Properties

[ Molecular Formula ]:
C23H33ClN4O3S

[ Molecular Weight ]:
481.05

[ Storage condition ]:
2-8℃

Related Compounds