DY131

Catalog No.S5364 Batch:S536402

Technical Data

Formula	C₁₈H₂₁N₃O₂
Molecular Weight	311.38	CAS No.	95167-41-2
Solubility (25°C)*	In vitro	DMSO	62 mg/mL (199.11 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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.

Cell Assay:^{^[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.

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.