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Formula | C22H22F3N3O3S2 |
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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.) |
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. | ||||
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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]. |
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.