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.
CAS Number: 95167-41-2
Molecular Weight: 311.38
Chemical Name: N'-[(1E)-[4-(diethylamino)phenyl]methylidene]-4-hydroxybenzohydrazide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C) DMSO: 62 mg/mL(199.11 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
DY131 is an ERRβ/γ-specific ligand that displays preferential selectivity for ERRγ at lower concentrations. It has no activity on the related receptors ERRα, ERα and ERβ. DY131 inhibits growth in a diverse panel of breast cancer cell lines, causing cell death that involves the p38 stress kinase pathway and a bimodal cell cycle arrest. ERRβ2 facilitates the block in G2/M, and DY131 delays progression from prophase to anaphase. ERRβ2 is a cytosolic protein that also localizes to centrosomes, and DY131 treatment leads to the appearance of multi- and monopolar spindles, thus causes mitotic spindle defects.
- Heckler MM, et al. Oncotarget. 2016, 7(30):47201-47220.
- Yu DD, et al. Bioorg Med Chem Lett. 2005, 15(5):1311-3.
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