I-BRD9

Catalog No.S7835 Batch:S783501

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Technical Data

Formula

C22H22F3N3O3S2

Molecular Weight 497.55 CAS No. 1714146-59-4
Solubility (25°C)* In vitro DMSO 99 mg/mL (198.97 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.)

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Biological Activity

Description I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 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[1].

Protocol (from reference)

Selleck's I-BRD9 has been cited by 9 publications

Bromodomain-Containing Protein 9 Regulates Signaling Pathways and Reprograms the Epigenome in Immortalized Human Uterine Fibroid Cells [ Int J Mol Sci, 2024, 25(2)905] PubMed: 38255982
Merkel cell polyomavirus small T antigen is a viral transcription activator that is essential for viral genome maintenance [ PLoS Pathog, 2022, 18(12):e1011039] PubMed: 36574443
Epigenetic and pharmacological control of pigmentation via Bromodomain Protein 9 (BRD9) [ Pigment Cell Melanoma Res, 2022, 10.1111/pcmr.13068] PubMed: 36112085
BRD9 is an essential regulator of glycolysis that creates an epigenetic vulnerability in colon adenocarcinoma [ Cancer Med, 2022, 10.1002/cam4.4954] PubMed: 35778964
BRD9 inhibition promotes PUMA-dependent apoptosis and augments the effect of imatinib in gastrointestinal stromal tumors [ Cell Death Dis, 2021, 12(11):962] PubMed: 34667163
SWI/SNF complex mutations promote thyroid tumor progression and insensitivity to redifferentiation therapies [ Cancer Discov, 2020, CD-20-0735] PubMed: 33318036
Everolimus enhances TRAIL-mediated anti-tumor activity of liver resident natural killer cells in mice [ Transpl Int, 2020, 33(2):229-243] PubMed: 31560810
Dynamic reversal of random X-Chromosome inactivation during iPSC reprogramming. [ Genome Res, 2019, 29(10):1659-1672] PubMed: 31515287
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193

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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.