DY-131


Catalog No. size PriceQuantity
M6405-2 2mg solid $94
M6405-10 10mg solid $360

Description

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.

Product information

CAS Number: 849764-85-8

Molecular Weight: 311.38

Formula: C18H21N3O2

Synonym:

GSK 9089

DY-131

DY 131

GSK9089

GSK-9089

Related CAS Number:

95167-41-2 (DY-131(EZ))

849764-85-8 (DY-131(E))

Chemical Name: N'-[(1E)-[4-(diethylamino)phenyl]methylidene]-4-hydroxybenzohydrazide

Smiles: CCN(CC)C1C=CC(/C=N/NC(=O)C2C=CC(O)=CC=2)=CC=1

InChiKey: WLKOCYWYAWBGKY-CPNJWEJPSA-N

InChi: InChI=1S/C18H21N3O2/c1-3-21(4-2)16-9-5-14(6-10-16)13-19-20-18(23)15-7-11-17(22)12-8-15/h5-13,22H,3-4H2,1-2H3,(H,20,23)/b19-13+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C) DMSO: 62 mg/mL(199.11 mM). Water: Insoluble.

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: ≥360 days 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

In Vitro:

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.

References:

  1. Heckler MM, et al. Oncotarget. 2016, 7(30):47201-47220.
  2. Yu DD, et al. Bioorg Med Chem Lett. 2005, 15(5):1311-3.

Products are for research use only. Not for human use.

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