| Mps1-IN-1Mps1 kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.11%
- COA (Certificate Of Analysis)
- HPLC
- MS (Mass Spectrometry)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Mps1-IN-1 Dilution Calculator
calculate
Mps1-IN-1 Molarity Calculator
calculate
| Cas No. | 1125593-20-5 | SDF | Download SDF |
| Chemical Name | 1-(4-((4-((2-(isopropylsulfonyl)phenyl)amino)-1H-pyrrolo[2,3-b]pyridin-6-yl)amino)-3-methoxyphenyl)piperidin-4-ol | ||
| Canonical SMILES | OC1CCN(C2=CC(OC)=C(NC3=NC4=C(C=CN4)C(NC5=C(S(=O)(C(C)C)=O)C=CC=C5)=C3)C=C2)CC1 | ||
| Formula | C28H33N5O4S | M.Wt | 535.66 |
| Solubility | ≥16.05mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
