DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.
体外研究
DY131 (0.1-30 μM; 5 days) treatment suppresses cell proliferation and reduces BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner, with higher suppression in LNCaP-ERRγ clone.
DY131inhibits Shh induced accumulation of Smo::EGFP with an IC50 of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC50 of ~2 μM.
DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh.
A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells.
Cell Proliferation Assay
Cell Line:
LNCaP-ERRγ and LNCaP cells
Concentration:
0.1 μM, 1 μM, 10 μM, 30 μM
Incubation Time:
5 days
Result:
Suppressed cell proliferation and reduced BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner.
体内研究
DY131 (5 μg/kg; subcutaneous injection; every second day; for 12 days) treatment increases P450 side-chain cleavage (P450scc), StAR and HMGCoA reductase (HMGCR) while decreases hormone sensitive lipase (HSL) expressions.
Animal Model:
Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g)
Dosage:
5 μg/kg
Administration:
Subcutaneous injection; every second day; for 12 days
Result:
Increased P450scc, StAR and HMGCR while decreased HSL expressions.
分子式
C18H21N3O2
分子量
311.38
CAS号
95167-41-2
运输条件
Room temperature in continental US; may vary elsewhere.