1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Kinesin
  3. CW-069

CW-069 

Cat. No.: HY-15857 Purity: 99.75%
Handling Instructions

CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.

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

CW-069 Chemical Structure

CW-069 Chemical Structure

CAS No. : 1594094-64-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Description

CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.

IC50 & Target[1]

HSET

75 μM (IC50)

In Vitro

CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM. CW-069 shows statistically significant selectivity over KSP. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC50 of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells[1].

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

Molecular Weight

500.33

Formula

C₂₃H₂₁IN₂O₃

CAS No.

1594094-64-0

SMILES

O=C(NC1=CC=C(I)C=C1C(O)=O)[[email protected]@H](NCC2=CC=CC=C2)CC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 52 mg/mL (103.93 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9987 mL 9.9934 mL 19.9868 mL
5 mM 0.3997 mL 1.9987 mL 3.9974 mL
10 mM 0.1999 mL 0.9993 mL 1.9987 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

The protocol is optimized for use with full-length, N-terminal, 6His-tagged HSET and KSP, and measured the MT-stimulated activity of the proteins. Inhibition of the Gsp synthetase activity of HSET/KSP is observed spectrophotometrically by coupling the hydrolysis of ATP to oxidation of NADH via pyruvate kinase/lactate dehydrogenase reactions. The assay is initiated by adding purified Gsp synthetase/amidase (12.8 nM) to an assay mixture containing the following components (final concentration): 6 nM protein, 0.07 mg/mL MTs, 1.56 mM glutathione, 10 mM spermidine, 2 mM ATP, 2.7 mM MgCl2, 1 mM phospho(enol)-pyruvate, 0.2 mM NADH, 50 μg/mL lactate dehydrogenase, 100 μg/mL pyruvate kinase, and various concentrations of inhibitor (CW-069) all in 50 mM Na PIPES (pH 6.8) at 37°C. The ADP-Glo detection assay is performed. All compound additions are performed using a multidrop BioMek Nxp. Plates are read using a Pherastar microplate reader[1].

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

Cell Assay
[1]

NHDF cells, HeLa cells, BT549, MCF-7 and MDA-MB-231 cells are verified by STR genotyping and all tested negative for mycoplasma. Cells are cultured in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C and 5% CO2. All compounds (CW-069) used in the Sulforhodamine B colorimetric (SRB) assay are dissolved in DMSO and diluted in culture medium to a final concentration of 0.2% DMSO. For the SRB assay and live-cell imaging, cells are seeded in 96-well plates at a density of 2,500 cells per well. After 24 hr, the cells are treated with compound (CW-069) for 72 hr, with triplicate wells for each concentration. For the SRB assay, the cells are then fixed with trichloroacetic acid (TCA) and stained with SRB. Fluorescence is quantified using an Infinite 200 PRO plate-reader at a wavelength of 545 nm. Compound (CW-069)-treated wells are compared with solvent control wells and the concentration of compound that resulted in 50% of the solvent-control cell growth is designated as the IC50 concentration, calculated using Graphpad PRISM 6. At least three biological replicates are performed for each assay[1].

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

References
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Keywords:

CW-069CW069CW 069KinesinInhibitorinhibitorinhibit

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CW-069
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