BTB-1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBTB-1Cat. No.: HY-101770CAS No.: 86030-08-2分式: CHClNOS分量: 297.71作靶点: Microtubule/Tubulin作通路: Cell Cycle/DNA Damage; Cytoskeleton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 DMSO : 100 mg/mL (33

2、5.90 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3590 mL 16.7949 mL 33.5897 mL5 mM 0.6718 mL 3.3590 mL 6.7179 mL10 mM 0.3359 mL 1.6795 mL 3.3590 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

3、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 (8.40 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.40 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn

4、 oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.40 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 BTB-1有效，选择性和可逆的有丝分裂运动蛋Kif18A的抑制剂，IC50值为1.69 M。IC50 & Target IC50: 1.69 M (Kif18A) 1体外研究 BTB-1 blocks the motility of Kif18A in a reversible manner. BTB-1 inhibits Kif18A in an a

5、denosinetriphosphate (ATP)-competitive but microtubule-uncompetitive manner and slows down the progression ofcells through mitosis. 100 M BTB-1 does not significantly inhibit any of the other tested mitotic kinesins.BTB-1 competes with ATP for Kif18A binding only when the motor-protein is associated

6、 with itspseudosubstrate microtubules. HeLa cells treated with BTB-1 accumulate in mitosis in a dose-dependentmanner 1. BTB-1 shows cell toxicity with an EC50 values of 35.8 M. HeLa cells treated with 50 M BTB-1reveals severe defects in spindle morphology and chromosome alignment. Treatment with hig

7、hconcentrations of BTB-1 does not result in elongated spindles 2.PROTOCOLKinase Assay 1 BTB-1 is prepared in DMSO. The activity of His-Kif18Amotor at increasing concentrations of ATP ismonitored in the presence of 3 M Mts and increasing concentrations of BTB-1 (0.21 M, 0.42 M, 0.85 M,1.7 M) or DMSO

8、as control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Catarinella M, et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6.2. Braun J, et al. Synthesis and biological evaluation of optimized inhibitors of the mitotic kinesin Kif18A. ACS Chem Biol. 2015 Feb20;10(2):554-60.McePdfHeightCaution: Product has not been fully validated for medical applica