Description
DY131 (95167-41-2) is a selective agonist at estrogen-related receptors ERRβ and ERRγ with minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.1?Displays antiproliferative activity in prostate cancer cells.2?Promotes hormone production and cell fusion in cytotrophoblasts.3?In breast cancer cells DY131 arrests cells in G2/M and causes mitotic spindle defects.4?Inhibits osteoclastogenesis and protects against inflammatory bone loss induced by LPS?in vivo.5
Uses
DY131 is a selective estrogen-related receptors (ERRβ and ERRγ) agonist (1,2). It is also an antimitotic agent that inhibits breast cancer cell growth.
Definition
ChEBI: N-[[4-(diethylamino)phenyl]methylideneamino]-4-hydroxybenzamide is a member of benzoic acids.
Biological Activity
Novel selective agonist at estrogen-related receptors ERR β and ERR γ . Displays minimal activity at ERR α , ER α and ER β at concentrations up to 30 μ M.
in vitro
dy131 was evaluated for its selectivity and efficacy in modulating the transcriptional activity of errα/β/γ and erβ/γ. cv-1 cells were transfected with reporter constructs or expression vectors and the fold activation of the reporter construct was determined at different concentrations of dy131. dy131 was found to be not able to activate the reporter construct or errα at any of the tested concentrations. in contrast, dy131 led to three- to fourfold activation of errβ at concentrations of 10-30 μm. activity on errγ was more pronounced with five-fold activation at 3 μm and maximal 6.6-fold activity observed at 30 μm. thus, dy131 was an selective errβ/γ ligand displaying preferential selectivity for errγ at lower concentrations [1].
References
1) Yu and Forman (2005),?Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma; Bioorg. Med. Chem. Lett.,?15?1311
2) Yu?et al.?(2008),?Orphan nuclear receptor estrogen-related receptor-beta suppresses in vitro and in vivo growth of prostate cancer cells via p21 (WAF1/CIP1) induction and as a potential therapeutic target in prostate cancer; Oncogene,?27?3313
3) Poidatz?et al. (2015),?Trophoblast syncytialisation necessitates mitochondrial function through estrogen-related receptor-τ; Mol. Hum. Reprod.,?21?206
4) Heckler?et al.?(2016),?Antimitotic activity of DY131 and the estrogen-related receptor beta 2 (ERR?2) splice variant in breast cancer; Oncotarget,?7?47201
5) Kim?et al.?(2019),?Estrogen-related receptor τ negatively regulates osteoclastogenesis and protects against inflammatory bone loss; J. Cell Physiol.,?234?1659
