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

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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 permeabilised and living cells, respectively.

Targets

PRMT5-RIOK1 complex (in permeabilized cells)	PRMT5-RIOK1 complex (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. This compound also reduces SDMA in the same subset of proteins affected by genetic perturbation of the PBM binding site.

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 with this compound. 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 with this compound. Twelve h later, cells are washed 1× with PBS and lysed on ice for 15 min in 50 μL lysis buffer.

References

https://pubmed.ncbi.nlm.nih.gov/34342224/

RETURN POLICY
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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.