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Chemical Structure| 1088965-37-0 Chemical Structure| 1088965-37-0

Structure of GSK-923295
CAS No.: 1088965-37-0

Chemical Structure| 1088965-37-0

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GSK-923295 is a specific allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki values of 3.2±0.2 nM and 1.6±0.1 nM for humans and canines, respectively.

Synonyms: GSK923295A

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Product Details of GSK-923295

CAS No. :1088965-37-0
Formula : C32H38ClN5O4
M.W : 592.13
SMILES Code : O=C(N[C@@H](CC1=CC=C(C2=CN3C=CC=C([C@@H](O)C)C3=N2)C=C1)CNC(CN(C)C)=O)C4=CC=C(OC(C)C)C(Cl)=C4
Synonyms :
GSK923295A
MDL No. :MFCD16038931
InChI Key :WHMXDBPHBVLYRC-OFVILXPXSA-N
Pubchem ID :46898058

Safety of GSK-923295

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK-923295

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • Kinesin

    CENP-E, Ki:3.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
A2780-cis cells 0.79 μM 72 hours Directly suppressed the growth of A2780-cis cells PMC6034569
HCT116 cells 2 μM approximately 2 weeks To screen for GSK-923295 resistant clones and analyze their resistance mechanisms PMC7444662
KBM7 cells 2 μM approximately 3 weeks To screen for GSK-923295 resistant clones and analyze their resistance mechanisms PMC7444662
GC-2 spd cells 100 nM siRNA 24 hours To study the role of CENP-E in spermatocyte division, found that CENP-E knockdown led to chromosome misalignment PMC7171076
breast cancer cell lines 0.0758 nM to 30 μM 72 hours To evaluate the effect of GSK-923295 on the growth of breast cancer cell lines, results showed that cell lines with high MNAI were more sensitive to GSK-923295. PMC4930593
A2780-cis ovarian cancer cells 0.79 μM 72 hours Directly suppressed the growth of A2780-cis cells PMC6034569
A549 cells 125 nM 48 hours To evaluate the antiproliferative activity of GSK923295 in combination with navitoclax, the results showed that the combination significantly enhanced cytotoxicity, mainly through inducing apoptosis. PMC10818680
NCI-H460 cells 125 nM 48 hours To evaluate the antiproliferative activity of GSK923295 in combination with navitoclax, the results showed that the combination significantly enhanced cytotoxicity, mainly through inducing apoptosis. PMC10818680
A549 cells 500 nM 48 hours To evaluate the cytotoxicity of BAY1217389 in combination with navitoclax, results showed that the combination treatment significantly increased apoptosis. PMC10818680
NCI-H460 cells 500 nM 48 hours To evaluate the cytotoxicity of BAY1217389 in combination with navitoclax, results showed that the combination treatment significantly increased apoptosis. PMC10818680

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ICR mice Testis injection 30 mg/kg Once daily for 14 days To study the effect of CENP-E inhibition on spermatogenesis in mice, found that CENP-E inhibition led to abnormalities in spermatogenesis PMC7171076

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00504790 Cancer Phase 1 Completed - United States, California ... More >> GSK Investigational Site Duarte, California, United States, 91010 United States, Michigan GSK Investigational Site Detroit, Michigan, United States, 48201 United States, Wisconsin GSK Investigational Site Madison, Wisconsin, United States, 53792-5666 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.44mL

1.69mL

0.84mL

16.89mL

3.38mL

1.69mL

References

 

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