BRD-4354 - HDAC 抑制剂 - 生命科学试剂 - 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作靶点: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Please store the product under the recommended conditions inthe COA.溶解性数据体外实验 DMSO : 125 mg/mL (326.46 mM; N

2、eed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根

3、据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.43 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.43 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.

4、43 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 BRD 4354是HDAC5 和 HDAC9 的抑制剂，其 IC50 值分别为 0.85，1.88 M。IC50 & Target HDAC5 HDAC90.85 M (IC50) 1.88 M (IC50)体外研究 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