Mps1-IN-1

Mps1 kinase inhibitor CAS# 1125593-20-5

Mps1-IN-1

Catalog No. BCC5590----Order now to get a substantial discount!

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Mps1-IN-1: 5mg $92 In Stock
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Chemical structure

Mps1-IN-1

3D structure

Chemical Properties of Mps1-IN-1

Cas No. 1125593-20-5 SDF Download SDF
PubChem ID 25195352 Appearance Powder
Formula C28H33N5O4S M.Wt 535.66
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 39 mg/mL (72.81 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[3-methoxy-4-[[4-(2-propan-2-ylsulfonylanilino)-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]phenyl]piperidin-4-ol
SMILES CC(C)S(=O)(=O)C1=CC=CC=C1NC2=CC(=NC3=C2C=CN3)NC4=C(C=C(C=C4)N5CCC(CC5)O)OC
Standard InChIKey NMJMRSQTDLRCRQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H33N5O4S/c1-18(2)38(35,36)26-7-5-4-6-23(26)30-24-17-27(32-28-21(24)10-13-29-28)31-22-9-8-19(16-25(22)37-3)33-14-11-20(34)12-15-33/h4-10,13,16-18,20,34H,11-12,14-15H2,1-3H3,(H3,29,30,31,32)
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.

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-1), 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].

Cell Assay [1]
U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block is performed using the following treatment regimen: thymidine for 18-20 hrs., release for 10 hrs. with doxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hours after the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cell populations is monitored with Cell Titer GLO assay[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-1 Dilution Calculator

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Mps1-IN-1 Molarity Calculator

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Preparing Stock Solutions of Mps1-IN-1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8669 mL 9.3343 mL 18.6686 mL 37.3371 mL 46.6714 mL
5 mM 0.3734 mL 1.8669 mL 3.7337 mL 7.4674 mL 9.3343 mL
10 mM 0.1867 mL 0.9334 mL 1.8669 mL 3.7337 mL 4.6671 mL
50 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.7467 mL 0.9334 mL
100 mM 0.0187 mL 0.0933 mL 0.1867 mL 0.3734 mL 0.4667 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-1

Mps1-IN-1 is a selective Mps1 (monopolar spindle 1) kinase inhibitor with IC50 value of 367 nM.

MPS1 (monopolar spindle 1 kinase) is a crucial part of the spindle assembly checkpoint. It facilitates the formation of C-MAD2 (closed MAD2) conformer and the MCC (mitotic checkpoint complex) assembly, involved in the maintenance of chromosomal stability and tumor growth.

Mps1-IN-1 abolishes the SAC (spindle assembly checkpoint) function. In U2OS cells, dose-dependent treatment of Mps1-IN-1 decreases the time spent in mitosis with almost 100% cells starting anaphase in 20 minutes. In contrast, just 10% of DMSO-treated cells starting anaphase in the same period. Acceleration of mitosis kinetics in Mps1-IN-1 treated cells affects genomic stability and causes aneuploidy. In addition, Mps1-IN-1 treated cells shows decrease in kinetochore-bound Mad2 by 80%. Mps1-IN-1–treated cells spent roughly 40% less time in mitosis as compared to DMSO-treated cells. Moreover, Mps1-IN-1 disrupts the kinase activity of Aurora B. Mps1-IN-1 treatment lead to decrease in the phosphorylation status of Aurora B at Thr232 in a dose-dependent manner. Furthermore, Mps1-IN-1 increases multipolar cell divisions and decreases cell viability.

Reference:
Kwiatkowski N, Jelluma N, Filippakopoulos P et al.  Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

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Description

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.

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