[CAS NO. 1714146-59-4] I-BRD9

Name: I-BRD9
Brand: Arctom Scientific
SKU: SLK-S7835

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PRODUCTS SPECIFICATIONS [1714146-59-4]

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Catalog

SLK-S7835

Brand

Selleck

CAS

1714146-59-4

DESCRIPTION [1714146-59-4]

Overview

MDL	-
Molecular Weight	497.55
Molecular Formula	C22H22F3N3O3S2
SMILES	N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

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Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0098 mL	10.0492 mL	20.0985 mL
5 mM	0.4020 mL	2.0098 mL	4.0197 mL
10 mM	0.2010 mL	1.0049 mL	2.0098 mL
50 mM	0.0402 mL	0.2010 mL	0.4020 mL

Description

I-BRD9 (GSK602) is a potent and selective inhibitor with of 7.3, while it displayed a pIC50 of 5.3 against BRD4.

Targets

BRD9 ^[1] (Cell-free assay)	BRD4 ^[1] (Cell-free assay)
7.3(pIC50)	5.3(pIC50)

In vitro

I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.

References

[1] Theodoulou NH, et al. J Med Chem. 2016, 59(4):1425-1439.