Mps1-IN-2

Mps1 kinase inhibitor CAS# 1228817-38-6

Mps1-IN-2

2D Structure

Catalog No. BCC4153----Order now to get a substantial discount!

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Quality Control of Mps1-IN-2

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3D structure

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Mps1-IN-2

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Chemical Properties of Mps1-IN-2

Cas No. 1228817-38-6 SDF Download SDF
PubChem ID 44968267 Appearance Powder
Formula C26H36N6O3 M.Wt 480.6
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 14.3 mg/mL (29.75 mM; Need ultrasonic and warming)
Chemical Name 9-cyclopentyl-2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5-methyl-7,8-dihydropyrimido[4,5-b][1,4]diazepin-6-one
SMILES CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(CCC(=O)N4C)C5CCCC5
Standard InChIKey WELBJLUKWAJOQV-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H36N6O3/c1-3-35-23-16-19(31-13-10-20(33)11-14-31)8-9-21(23)28-26-27-17-22-25(29-26)32(18-6-4-5-7-18)15-12-24(34)30(22)2/h8-9,16-18,20,33H,3-7,10-15H2,1-2H3,(H,27,28,29)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Mps1-IN-2

DescriptionMps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.In Vitro:Mps1-IN-2 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 145 nM and 12 nM. Mps1-IN-2 also shows high affinity for PLK1 and GAK with Kds of 61 and 140 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-2 can induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells[1].

References:
[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

Protocol

Kinase Assay [1]
The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-2), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay[1].

References:
[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

Mps1-IN-2 Dilution Calculator

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Preparing Stock Solutions of Mps1-IN-2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0807 mL 10.4037 mL 20.8073 mL 41.6146 mL 52.0183 mL
5 mM 0.4161 mL 2.0807 mL 4.1615 mL 8.3229 mL 10.4037 mL
10 mM 0.2081 mL 1.0404 mL 2.0807 mL 4.1615 mL 5.2018 mL
50 mM 0.0416 mL 0.2081 mL 0.4161 mL 0.8323 mL 1.0404 mL
100 mM 0.0208 mL 0.104 mL 0.2081 mL 0.4161 mL 0.5202 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Mps1-IN-2

Mps1-IN-2 is a potent and selective ATP-competitive inhibitor of Mps1 kinase with the IC50 value of 145nM [1].

Mps1-IN-2 has been reported to inhibit Mps1 kinase activity with the IC50 value of 145nM, when screened at 1μM ATP. In addition, Mps1-IN-2 has shown greater than 1000-fold selectivity to the Alk and Ltk enzyme. Moreover, Mps1-IN-2 has been revealed to bound to the ATP biding pocket of Mpa1 and formed a hydrogen bond with the hinge backbone (Glu603) at 2.74-Å resolution. Mps1-IN-2 has been noted to abrogate SAC function and override the checkpoint through direct inhibition of Mps1[1].

References:
[1] Kwiatkowski N1, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. doi: 10.1038/nchembio.345. Epub 2010 Apr 11.

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Description

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.

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