BRD0539

製品コードS8844 バッチS884401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₂₅FN₂O₃S

分子量

452.54

CAS No.

1403838-79-8

Solubility (25°C)*

体外

DMSO

91 mg/mL (201.08 mM)

Ethanol

31 mg/mL (68.5 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.550mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 91 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.750mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	BRD0539 is a potent inhibitor of spCas9 which disrupts spCas9-DNA binding and exerts dose and temporal control of spCas9 in human cell lines.
in vitro	BRD0539 is stable in human plasma and reversibly inhibits SpCas9. This compound does not interfere with the SpCas9:gRNA interaction. It dose-dependently blocks the formation of the DNA-bound state in a dose-dependent fashion. It impairs the perturbation induced by the 4PAM DNA. It is able to inhibit SpCas9 in the eGFP-disruption assay.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U2OS.eGFP.PEST cells
	濃度	15 μM
	反応時間	2–24 h
	実験の流れ	The reversal of BRD0539-mediated inhibition of SpCas9 is performed using the eGFP-disruption assay, wherein 2×10⁵ U2OS.eGFP.PEST cells are nucleofected with preformed SpCas9:gRNA complex. Approximately 22,000 transfected cells/well are plated in four replicates in a 96-well plate along with 15 μM of this compound or DMSO. For AcrIIA4 reversibility experiments, a preformed SpCas9:gRNA (10 pmol) is incubated with AcrIIA4 (5×) for 10 min and then is nucleofected to U2OS.eGFP.PEST cells following the aforementioned protocol. The media is swapped with fresh media containing no this chemical/AcrIIA4 at the indicated time point (2–24 h), and the cells are allowed to grow until 24 h post-nucleofection.

参考

https://pubmed.ncbi.nlm.nih.gov/31051099/

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：

Targeting KDM4A epigenetically activates tumor-cell-intrinsic immunity by inducing DNA replication stress [ Mol Cell, 2021, S1097-2765(21)00168-4]	PubMed: 33743195

Targeting KDM4A epigenetically activates tumor-cell-intrinsic immunity by inducing DNA replication stress [ Mol Cell, 2021, S1097-2765(21)00168-4]

PubMed: 33743195

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。