BRD-4354 - HDAC 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBRD 4354Cat. No.: HY-112719CAS No.: 315698-07-8分式: CHClNO分量: 382.89作靶點: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (326.46 mM; N

2、eed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6117 mL 13.0586 mL 26.1172 mL5 mM 0.5223 mL 2.6117 mL 5.2234 mL10 mM 0.2612 mL 1.3059 mL 2.6117 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根

3、據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.43 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.43 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.

4、43 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 BRD 4354是HDAC5 和 HDAC9 的抑制劑，其 IC50 值分別為 0.85，1.88 M。IC50 & Target HDAC5 HDAC90.85 M (IC50) 1.88 M (IC50)體外研究 BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with BRD4354 having half-maximuminh

5、ibitory concentrations (IC50) of 0.85 M and 1.88 M, respectively. BRD 4354 also inhibits HDACs 4, 6, 7,and 8 at higher concentrations (3.88-13.8 M) but demonstrates less of an inhibitory effect on other class IHDACs 1, 2, and 3 (IC5040 M) 1.PROTOCOLCell Assay 1 A549 adenocarcinoma cells were treated

6、 with BRD 4354 for 24 h at 10 M, and the top 50 upregulated andtop 50 down regulated genes are compared to other compound treatments involving drugs, bioactivecompounds with established MoA, and novel synthetic compounds 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Boskovic ZV, ET AL. Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. ACS Chem Biol. 2016Jul 15;11(7):1844-51.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl