1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Kinesin

GSK-923295 

Cat. No.: HY-10299 Purity: >99.0%
Handling Instructions

GSK-923295 is a special, allosteric inhibitor of CENP-E kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.

For research use only. We do not sell to patients.
GSK-923295 Chemical Structure

GSK-923295 Chemical Structure

CAS No. : 1088965-37-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 172 In-stock
5 mg USD 132 In-stock
10 mg USD 216 In-stock
50 mg USD 756 In-stock
100 mg USD 1320 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    GSK-923295 purchased from MCE. Usage Cited in: Cancer Lett. 2015 May 28;361(1):97-103.

    Apoptotic effects of GSK923295 on MESSA and MESSA Dx5 cells. MESSA and MESSA Dx5 cells are treated with Verapamil (20 μM), GSK923295 (4 μM), and combination GSK923295 (4 μM) plus Verapamil (20 μM) for 24 h. Actin is used as loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GSK-923295 is a special, allosteric inhibitor of CENP-E kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.

    IC50 & Target

    Ki: 3.2 nM (human CENP-E), 1.6 nM (canine CENP-E)[1]

    In Vitro

    GSK-923295 (GSK923295) is a first-in-class, specific, allosteric inhibitor of CENP-E kinesin motor function. GSK923295 is uncompetitive with both ATP and MT, inhibiting CENP-E MT-stimulated ATPase activity with a Ki of 3.2±0.2 nM and 1.6±0.1 nM for human and canine, respectively. GSK923295 inhibits release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules[1]. GSK923295 has broad growth inhibitory activity in a panel of 237 cancer cell lines and produces significant tumor growth-delay in 8 of the 11 mouse xenograft tumor models with IC50s of 17.2 nM, 55.6 nM, 42 nM, and 51.9 nM for SW48, RKO (BRAF mutant), SW620 (KRAS mutant), and HCT116 (KRAS mutant), respectively[2]. GSK923295 is a potent and selective small molecule inhibitor of human CENPE with a Ki of 3.2 nM. GSK923295 demonstrates broad efficacy against a panel of 19 human neuroblastoma derived cell lines with an average growth IC50 of 41 nM[3].

    In Vivo

    Xenografts of mice treated with GSK-923295 (GSK923295) shows significant tumor growth delay compared to the control arm (NB-EBc1 p<0.0001; NB-1643 p=0.018; NB-1691 p=0.0018)[3].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.6888 mL 8.4441 mL 16.8882 mL
    5 mM 0.3378 mL 1.6888 mL 3.3776 mL
    10 mM 0.1689 mL 0.8444 mL 1.6888 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    GSK-923295 (GSK923295) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    Cell-growth inhibition assays are performed by MDS in 384-well plates, and DNA content of fixed cells stained with DAPI using an Incell 1000 (GE) is analyzed. DNA content is determined 24 h after seeding (T0) and after exposure to varying concentrations of GSK-923295 (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, and 100 μM) for an additional 72 h (T72). All T72 measurements are normalized to T0. Curves are analyzed using the XLfit curve-fitting tool to determine the concentration of GSK923295 yielding 50% growth inhibition relative to T0 and Ymax values (GI50)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    GSK-923295 (GSK923295) is prepared in 96% acidified water, 2% DMAC, and 2% CREM (Mice)[3].

    Mice[3]
    CB17 scid mice are used to propagate subcutaneously implanted neuroblastoma tumors. Tumor diameters are measured using calipers. Tumor volumes are calculated. Once tumor volume exceeds 200 mm3, mice are randomized (n=10 per arm) to receive either GSK923295 125 mg/kg IP or vehicle (96% acidified water, 2% DMAC, 2% CREM) for a total of 6 doses using a 3 days on, 4 days off, 3 days on regimen. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    592.13

    Formula

    C₃₂H₃₈ClN₅O₄

    CAS No.

    1088965-37-0

    SMILES

    O=C(N[[email protected]@H](CC1=CC=C(C2=CN3C(C([[email protected]@H](O)C)=CC=C3)=N2)C=C1)CNC(CN(C)C)=O)C4=CC(Cl)=C(C=C4)OC(C)C

    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

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    GSK-923295
    Cat. No.:
    HY-10299
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