ER covalent antagonist-1

ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα) . ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model[1].

Product Specifications

CAS Number

[2757498-74-9]

UNSPSC

12352005

Target

Apoptosis; Estrogen Receptor/ERR

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Field of Research

Cancer

Smiles

O=C(C1=CC=CC=C1)C(SC2=CC(O)=CC=C23)=C3OC4=CC=C(C=C4)OC5CN(C5)C/C=C/C(N6CCCCC6)=O

Molecular Formula

C33H32N2O5S

Molecular Weight

568.68

References & Citations

[1]Bai C, et al., X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles. Bioorg Chem. 2023 Dec;141:106919.