Estrogen receptor β antagonist 2

Names

[ CAS No. ]:
2580941-14-4

[ Name ]:
Estrogen receptor β antagonist 2

Biological Activity

[Description]:

Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer

[Target]

ERα:109.10 μM (IC50)

ERβ:0.63 μM (IC50)


[In Vitro]

Estrogen receptor β antagonist 2 (compound 42) (0-100 µM) shows antiproliferative activity with IC50 value of >100 µM in MCF-7cells[1]. .Estrogen receptor β antagonist 2 exhibits differences in interaction potential to H12 of ERβ via Asp303 (H3) H-bonding to Tyr488[1].

[References]

[1]. Carr M, et al. Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. Bioorg Med Chem. 2020 Mar 1;28(5):115261.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H26N2O6

[ Molecular Weight ]:
426.46

Related Compounds