I-BRD9

製品コードS7835 バッチS783502

印刷

化学情報

Synonyms

GSK602

Storage
(From the date of receipt)

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

化学式

C₂₂H₂₂F₃N₃O₃S₂

分子量

497.55

CAS No.

1714146-59-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (200.98 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml
	5% DMSO 1 95% Corn oil	1.65mg/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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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].

製品説明

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.

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].

プロトコル(参考用のみ)

参考

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。