DY131

Catalog No.S5364

For research use only.

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).

DY131 Chemical Structure

CAS No. 95167-41-2

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

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Biological Activity

Description DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).
Targets
ERRβ [1]
()
ERRγ [1]
()
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[1]. 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[2].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: MDA-MB-231 and MCF-7 cells
  • Concentrations: 2.5, 5 and 10 μM
  • Incubation Time: 18-24 h
  • Method:

    On day 0, 150 (MDA-MB-231) or 200 (MCF7) cells were seeded per well in 4 wells of a 12-well plastic tissue culture dish. The following day, indicated concentrations of DY131 were added for 18-24 h. On day 2, drug containing media were removed, wells were washed with 1X PBS, and fresh media (no drug) was added to the wells. Cells were cultured in the absence of drug for an additional 13 d, changing media twice, before staining with crystal violet solution.

Solubility (25°C)

In vitro

DMSO 62 mg/mL
(199.11 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 311.38
Formula

C18H21N3O2

CAS No. 95167-41-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)C1=CC=C(C=C1)C=NNC(=O)C2=CC=C(C=C2)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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