BRD0639

Catalog No.E1007 Batch:E100701

Technical Data

Formula	C₂₁H₂₂ClN₅O₄S
Molecular Weight	475.948	CAS No.	2760881-74-9
Solubility (25°C)*	In vitro	DMSO	95 mg/mL (199.6 mM)
		Ethanol	95 mg/mL (199.6 mM)
		Water	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

BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively.

Targets

PRMT5-RIOK1 complex ^[1] (in permeabilized cells)	PRMT5-RIOK1 complex ^[1] (in permeabilized cells)
7.5 μM	16 μM

In vitro

BRD0639, which engages the target in Expi293 cells, disrupts PRMT5−RIOK1 complexes, and reduces substrate methylation. BRD0639 also reduces SDMA in the same subset of proteins affected by genetic perturbation of the PBM binding site.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Expi293 cells Concentrations 25 μM Incubation Time 12 h Method Cells are plated at 1 × 10⁶/well in 6-well tissue culture treated plates and treated the next day with BRD0639 to a final concentration of 25 μM. Twelve h after treatment, the media is refreshed and cells retreated. Twelve h later, cells are washed 1× with PBS and lysed on ice for 15 min in 50 μL lysis buffer.

Cell Assay:^{^[1]}

Cell lines
Expi293 cells
Concentrations
25 μM
Incubation Time
12 h
Method
Cells are plated at 1 × 10⁶/well in 6-well tissue culture treated plates and treated the next day with BRD0639 to a final concentration of 25 μM. Twelve h after treatment, the media is refreshed and cells retreated. Twelve h later, cells are washed 1× with PBS and lysed on ice for 15 min in 50 μL lysis buffer.

References

[1] David C McKinney, et al. J Med Chem . 2021 Aug 12;64(15):11148-11168.

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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.

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