DY-131

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DY131 是一种新型选择性 ERRβ 和 ERRγ 激动剂。

DY131, also known as GSK-9089, is a novel selective agonist at estrogen-related receptors ERRβ and ERRγ. DY131 could potentiate the ERRgamma-induced growth inhibition in LNCaP-ERRgamma and DU145-ERRgamma cells in a dose-dependent manner. ERRgamma may perform an antiproliferative or tumor-suppressing function in prostate cancer cells. ERRgamma could be a novel therapeutic target for prostate cancer treatment.

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.DY131 inhibits 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.

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.

DY131 | DY-131 | DY 131 | GSK-9089

Tyrosine Kinase

Ephrin Receptor

ERRβ| ERRγ

Cancer

——

95167-41-2

311.38

C18H21N3O2

>98% (HPLC)

DMSO : 50 mg/mL. 160.58 mM;

C(=O)(c1ccc(cc1)O)N/N=C/c1ccc(cc1)N(CC)CC

(E)-N'-(4-(diethylamino)benzylidene)-4-hydroxybenzohydrazide

(-20℃)

With Ice Pack

≥ 2 years