533884-09-2

533884-09-2 structure

Name: LY500307
Chemical Name: (3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
CAS Number: 533884-09-2
Molecular Formula: C₁₈H₁₈O₃
Molecular Weight: 282.33
Catalog: Biochemical Inhibitor Endocrinology & Hormones Estrogen/progestogen Receptor agonist
Create Date: 2018-12-18 10:21:05
Modify Date: 2024-01-31 19:28:43
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].

Name	(3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
Synonyms	Erteberel (3aS,4R,9bR)-4-(4-Hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol Benzo[b]cyclopenta[d]pyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aS,4R,9bR)- (3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta[c][1]benzopyran-8-ol LY500307

Description	Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Neurological Disease
Target	Ki: 1.54 nM (ERβ)[1] EC50: 3.61 nM[1]
In Vitro	Treatment with LY500307 significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2]. ERβ agonists promote apoptosis of GBM cells. It modulated several pathways related to apoptosis, cell cycle, and DNA damage response[2]. LY500307 sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide[2].
In Vivo	LY500307 treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model[2]. LY500307 treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model[2].
References	[1]. Zhao L, et al. Pharmacological activation of estrogen receptor beta augments innate immunity to suppress cancer metastasis. Proc Natl Acad Sci U S A. 2018 Apr 17;115(16):E3673-E3681. [2]. Sareddy GR, et al. Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma. Sci Rep. 2016 Apr 29;6:24185.