Hesperadin - Aurora Kinase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHesperadinCat. No.: HY-12054CAS No.: 422513-13-1分式: CHNOS分量: 516.65作靶点: Aurora Kinase; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DM

2、SO : 100 mg/mL (193.55 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9355 mL 9.6777 mL 19.3555 mL5 mM 0.3871 mL 1.9355 mL 3.8711 mL10 mM 0.1936 mL 0.9678 mL 1.9355 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

3、，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: 2.5 mg/mL (4.84 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.84 mM); Clear solution1/3 Master of Small Molecul

4、es 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Hesperadin是ATP竞争型的极光激酶 (aurora B) 抑制剂，IC50值为250 nM。IC50 & Target Aurora B250 nM (IC50)体外研究 Hesperadin also inhibits other kinases such as AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK at 1 Mdrug concentration. Hesperadin causes polyploidy in HeLa cells. Hespe

5、radin-treated HeLa cells showalignment and segregation defects, but sister chromatid separation is intact. Hesperadin causes defects inmitosis and cytokinesis. Hesperadin inhibits Aurora B. Immunofluorescence microscopy reveals thatHesperadin-treated cells in which chromosomes are stretched toward o

6、pposite poles, i.e., which haveentered anaphase, fail to assemble a central spindle and to properly localize the human centralspindlinsubunits CYK-4 and MKLP1 1. Hesperadin inhibits multiple human clinical isolates of influenza A and Bviruses with single to submicromolar efficacy, including oseltami

7、vir-resistant strains. Mechanistic studiesreveal that hesperadin inhibits the early stage of viral replication by delaying the nuclear entry of viralribonucleoprotein complex, thereby inhibiting viral RNA transcription and translation as well as viral proteinsynthesis 2. Hesperadin inhibits cell cel

8、l proliferation due to appearance of multiple mitotic defects causedby Aurora B activity reduction and elimination of checkpoint proteins-such as hBUBR1 and CENP-E-fromkinetochores of mitotic chromosomes 3.PROTOCOLKinase Assay 1 The kinase assay is performed with 10 L beads in 20 L kinase buffer con

9、taining 5 g histone H1, 1 M ATP,1 Ci 32PATP, and the appropriate concentration of Hesperadin or DMSO for 30 min at 37C. SDS samplebuffer is added, and samples are boiled and resolved by SDS. The gel is dried, and the radioactivesignal is detected by PhosphorImager analysis 1.MCE has not independentl

10、y confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 To determine cellular cytotoxicity of Hesperadin, 200 L fresh DMEM (without FBS) medium containing serialhalf-log diluted Hesperadin is added to each well. After incubating for 48 h with 5% CO2 in the cell cultureinc

11、ubator at 37 C, the medium is removed and 100 L DMEM medium containing 40 g/mL neutral red isadded. The solution is incubated for another 4 h at 37 C in the cell culture incubator. The medium isremoved and the amount of neutral red that is taken by the viable cells is dissolved by adding 100 L ofdes

12、taining solution (50% ethanol, 49% H2O, and 1% acetic acid). The absorbance of the solution at 540 nmis determined 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Hauf S, et al. The small molecule Hesperadin reveals a role for Aurora B in

13、 correcting kinetochore-microtubule attachment and inmaintaining the spindle assembly checkpoint. J Cell Biol. 2003 Apr 28;161(2):281-94.2. Hu Y, et al. Chemical Genomics Approach Leads to the Identification of Hesperadin, an Aurora B Kinase Inhibitor, as a Broad-Spectrum2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEInfluenza Antiviral. Int J Mol Sci. 2017 Sep 8;18(9).3. Ladygina NG, et al. Effect of the pharmacological agent hesperadin on breast and prostate tumor cultured cells. Biomed Khim. 2005Mar-Apr;51(2):17