PFI-4

製品コードS7906 バッチS790601

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H24N4O3
分子量 380.44 CAS No. 900305-37-5
Solubility (25°C)* 体外 DMSO 17 mg/mL warmed with 50ºC water bath (44.68 mM)
Ethanol 5 mg/mL warmed with 50ºC water bath (13.14 mM)
Water 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
in vitro PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3. [1]

プロトコル(参考用のみ)

キナーゼアッセイ BRPF1, 2 and 3 TR-FRET assays
Compounds are screened against 6H-Flag-Tev-BRPF1 (622-738), 6HisFlag-Tev-BRPF2 (also known as BRD1) (551-673) or 6His-Flag-Tev-BRPF3 (579-706) protein in dose-response format in a TR-FRET assay measuring competition between test compound and a synthetic fluorescent ligand. Compounds are titrated from 10 mM in 100% DMSO and 100 nL transferred to a low volume black 384 well micro titre plate using a Labcyte Echo 555. A Thermo Scientific Multidrop Combi is used to dispense 5 μL of 4 nM BRPF1, 20 nM BRPF2 or 40 nM BRPF3 protein respectively in an assay buffer of 50 mM HEPES, 150 mM NaCl, 5% glycerol, 1mM DTT and 1 mM CHAPS, pH 7.4, and in the presence of the appropriate fluorescent ligand concentration (~Kd concentration for the interaction between protein and ligand). After equilibrating for 30 mins in the dark at rt, the bromodomain protein:fluorescent ligand interaction is detected using TR-FRET following a 5 μL addition of either 3 nM Lanthascreen Elite Tb-anti His antibody for the Alexa 488 ligands, or 3 nM europium chelate labelled anti-6His antibody (Perkin Elmer, W1024, AD0111) for the Alexa 647 ligand, in assay buffer. Time resolved fluorescence energy transfer (TR-FRET) is then detected on a time-resolved fluorescence laser equipped Perkin Elmer Envision multimode plate reader using the appropriate protocol (excitation = 337 nm; emission 1 Alexa 488 = 495 nm; emission 2 Alexa 488 = 520 nm, emission 1 Alexa 647 = 615 nm; emission 2 Alexa 647= 665 nm ). TR-FRET ratio is calculated using the following equation: Ratio = ((Acceptor fluorescence at 520 or 665 nm) / (Donor fluorescence at 495 or 615 nm)) * 1000. Data are analysed as for the BRD4 assay.

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：

Isoform-specific Involvement of Brpf1 in Expansion of Adult Hematopoietic Stem and Progenitor Cells [ J Mol Cell Biol, 2020, 11;12(5):359-371] PubMed: 31565729

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。

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