2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. Mps1-IN-1 dihydrochloride

Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells.

For research use only. We do not sell to patients.

Mps1-IN-1 dihydrochloride Chemical Structure

Mps1-IN-1 dihydrochloride Chemical Structure

CAS No. : 1883548-93-3

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Based on 1 publication(s) in Google Scholar

Mps1-IN-1 dihydrochloride Related Antibodies

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Description

Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells[1].

IC50 & Target[1]

Mps1

367 nM (IC50)

Mps1

27 nM (Kd)

ALK

21 nM (Kd)

LTK

29 nM (Kd)

PYK2

280 nM (Kd)

FAK

440 nM (Kd)

IGF1R

750 nM (Kd)

INSR

470 μM (Kd)

CLK1

1900 nM (Kd)

ERK2

2900 nM (Kd)

INSRR

1200 nM (Kd)

TNK1

2600 nM (Kd)

TNK2

3100 nM (Kd)

GAK

1100 nM (Kd)

In Vitro

Mps1-IN-1 dihydrochloride (2-10 μM; 96 hours) inhibits the proliferative capacity of HCT116 cells to 33% that of DMSO control[1].
Mps1-IN-1 dihydrochloride (0.3-10 μM; 4 hours) induces bypass of a checkpoint-mediated mitotic arrest in a dose-dependent manner. Mps1-IN-1 dihydrochloride (10 µM) administration results in a dose-dependent decrease in the time spent in mitosis with nearly 100% U2OS cells initiating anaphase within 20 minutes[1].
Mps1-IN-1 dihydrochloride (0.5, 2, 10 μM) causes a dose-dependent reduction in hyper-phosphorylated Mps1 as demonstrated by a decrease in phosphorylation-induced mobility shift in UTRM10 LAP-Mps1 WT cells[1].
Mps1-IN-1 (5, 10 μM) arrested in mitosis using Nocodazole, results in a dose-dependent accumulation of 4c pHistone H3 negative cells in U2OS cells[1].
Acceleration of mitosis kinetics in Mps1-IN-1-treated cells had direct consequences on genomic stability with cells exhibiting significant signs of chromosome mis-alignment and chromosome mis-segregation[1].
Mps1-IN-1 dihydrochloride demonstrates greater than 1000-fold selectivity relative to the 352 member kinase panel with the major exceptions of Alk and Ltk[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Mps1-IN-1 dihydrochloride Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 2, 5, 10 μM
Incubation Time: 96 hours
Result: The proliferative capacity of HCT116 cells was reduced to 33% that of DMSO control.

Cell Cycle Analysis[1]

Cell Line: U2OS cells
Concentration: 0.3, 0.5, 1, 2, 5, 10 μM
Incubation Time: 4 hours
Result: Dropped levels of cyclin B protein, which accumulate in G2 and are sustained during an activated spindle checkpoint.

Western Blot Analysis[1]

Cell Line: Hela and U2OS cells
Concentration: 10 μM
Incubation Time: Pretreatment 1 hour before taxol and MG132
Result: Caused a dose-dependent reduction in the phosphorylation status of Aurora B at threonine-232 (Thr232).
Molecular Weight

608.58

Formula

C28H35Cl2N5O4S
CAS No.
SMILES

OC1CCN(C2=CC=C(NC3=CC(NC4=CC=CC=C4S(=O)(C(C)C)=O)=C5C(NC=C5)=N3)C(OC)=C2)CC1.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Mps1-IN-1 dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mps1-IN-11883548-93-3Mps1Monopolar spindle 1ATPmitoticabrogatesspindleassemblycheckpointSACHCT116AlkLtkTTKU2OSInhibitorinhibitorinhibit

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