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I-BRD9

Catalog No. T6859 CAS 1714146-59-4

Synonyms: GSK602

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

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I-BRD9, CAS 1714146-59-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 115.00
25 mg	In stock	$ 227.00
50 mg	In stock	$ 433.00
100 mg	In stock	$ 642.00
1 mL * 10 mM (in DMSO)	In stock	$ 76.00

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Purity: 99.28%

Purity: 99.05%

Purity: 98.16%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.
Targets&IC50	BRD9:7.3 (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[1].
Kinase Assay	Receptor binding is performed using membranes prepared from cells with recombinant expression of adenosine receptors as follows: human A2A and HEK 293, rat A2A and Chinese hamster ovary, human and rat A1 and Chinese hamster ovary, and human A3 and HEK 293. Radioligand competition binding assays are performed in 96-well plates in a total assay volume of 200 μL using a final test drug concentration range of between 0.1 and 3 μM. Membranes are diluted in assay buffer, pH 7.4 (A1 and A2A, Dulbecco's phosphate-buffered saline with 10 mM MgCl2; A3, 50 mM Tris-HCl, 120 mM NaCl, 10 mM MgCl2). To remove endogenous adenosine from the membrane preparations, 4 U/mL adenosine deaminase is added to the membranes, which are then incubated at room temperature for 15 min. Radioligand is added to a final concentration of 0.5 ([3H]SCH 58261, A2A), 1 ([3H]DPCPX, A1), or 0.25 ([125I]AB-MECA, A3) nM. Nonspecific binding is defined by adding 100 nM CGS 15923 (A2A), 100 nM NECA (A1), or 100 nM DPCPX (A3). Plates are incubated at room temperature with agitation for 1.5 h (A2A and A1) or 2 h (A3). Membranes are filtered onto Packard GF-B filter plates and washed in ice-cold assay buffer using a Brandel cell harvester to separate bound and free radioligand. The plates are dried before addition of 45 μL of Microscint 20 to each well.

Synonyms	GSK602
Molecular Weight	497.55
Formula	C22H22F3N3O3S2
CAS No.	1714146-59-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (100.49 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library Fluorochemical Library Histone Modification Compound Library Reprogramming Compound Library Chromatin Modification Compound Library Bioactive Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max

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Keywords

I-BRD9 1714146-59-4 Chromatin/Epigenetic Epigenetic Reader Domain cancer inhibit bromodomain-containing protein 7(BRD7) bromodomain and extra terminal domain (BET) BRD9 GSK 602 Kasumi-1 cells Inhibitor GSK-602 GSK602 probe I-BRD-9 I BRD9 immune response IBRD9 inhibitor

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