Mps1-IN-1 - Mps1 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMps1-IN-1Cat. No.: HY-13298CAS No.: 1125593-20-5分式: CHNOS分量: 535.66作靶点: Mps1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 : 39 mg/mL (72.81 mM)* mean

2、s soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8669 mL 9.3343 mL 18.6686 mL5 mM 0.3734 mL 1.8669 mL 3.7337 mL10 mM 0.1867 mL 0.9334 mL 1.8669 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。BIOLOGICAL ACTIVITY物活性 Mps1-IN-1种有效的，选择性的，ATP 竞争性的 Mps1 抑制剂，IC50 和 Kd 值分

3、别为 367 nM 和 27 nM。IC50 & Target Mps1 ALK LTK PYK227 nM (Kd) 21 nM (Kd) 29 nM (Kd) 280 nM (Kd)FAK IGF1R INSR CLK11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE440 nM (Kd) 750 nM (Kd) 470 nM (Kd) 1900 nM (Kd)ERK2 INSRR TNK1 TNK22900 nM (Kd) 1200 nM (Kd) 2600 nM (Kd) 3100 nM (Kd)GAK1100 nM (Kd)体外研究

4、Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with Kds of 21 and 39 nM, respectively,but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 M) induces b

5、ypass of acheckpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores,and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 M) shows noeffect on centrosome duplication. In addition, Mps1-IN-1 (5-10 M) suppresses the p

6、roliferative capacity ofHCT116 1.PROTOCOLKinase Assay 1 The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of afluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each15 L assay contains 5 nM TTK, varia

7、ble amounts of test compound (Mps1-IN-1), 30 nM Kinase Tracer 236,2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mMHEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 Lof test compound (from 2-fold dilut

8、ion series) to 5 L of a kinase/antibody mixture, followed by addition of 5 L of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measuredover a 200 s window

9、 following a 100 s post-excitation delay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block isperformed using the following treatment reg

10、imen: thymidine for 18-20 hrs., release for 10 hrs. withdoxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hoursafter the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cellpopulations is monitored with Ce

11、ll Titer GLO assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.McePdfHeightCaution: Product has not be