1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Mps1
    Polo-like Kinase (PLK)

Mps1-IN-2 

Cat. No.: HY-13994 Purity: 98.06%
Handling Instructions

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.

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

Mps1-IN-2 Chemical Structure

Mps1-IN-2 Chemical Structure

CAS No. : 1228817-38-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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View All Polo-like Kinase (PLK) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

Mps1

12 nM (Kd)

GAK

140 nM (Kd)

PLK1

61 nM (Kd)

PLK3

1600 nM (Kd)

PLK4

3100 nM (Kd)

STK33

5000 nM (Kd)

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].

Solvent & Solubility
In Vitro: 

DMSO : 14.3 mg/mL (29.75 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0807 mL 10.4037 mL 20.8073 mL
5 mM 0.4161 mL 2.0807 mL 4.1615 mL
10 mM 0.2081 mL 1.0404 mL 2.0807 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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].

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

References
Molecular Weight

480.60

Formula

C₂₆H₃₆N₆O₃

CAS No.

1228817-38-6

SMILES

CN(C1=CN=C(NC2=C(OCC)C=C(N3CCC(O)CC3)C=C2)N=C1N(C4CCCC4)CC5)C5=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
Mps1-IN-2
Cat. No.:
HY-13994
Quantity:

Mps1-IN-2

Cat. No.: HY-13994