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GSK-923295

Catalog No. T2039   CAS 1088965-37-0

GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM).

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GSK-923295 Chemical Structure
GSK-923295, CAS 1088965-37-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 45.00
2 mg In stock $ 64.00
5 mg In stock $ 98.00
10 mg In stock $ 177.00
25 mg In stock $ 349.00
50 mg In stock $ 537.00
100 mg In stock $ 775.00
1 mL * 10 mM (in DMSO) In stock $ 138.00
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Purity: 99.71%
Purity: 98%
Purity: 96.22%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM).
Targets&IC50 CENP-E:3.2 nM(Ki)
Kinase Assay Enzymology: Kinesin motor domains are expressed in Escherichia coli BL21(DE3) and purified. CENP-E proteins includes residues 2–340 with a carboxyl-terminal 6-his tag. All studies using MT are conducted in PEM25 buffer [25 mM PipesK+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM MT, and 1 nM CENP-E in PEM25 buffer.
Cell Research 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 is analyzed. DNA content is determined 24 h after seeding (T0) and after exposure to varying concentrations of drug 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).(Only for Reference)
Molecular Weight 592.13
Formula C32H38ClN5O4
CAS No. 1088965-37-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (157.1 mM)

DMSO: 93 mg/mL (157.1 mM)

TargetMolReferences and Literature

1. Wood KW, et al. Proc Natl Acad Sci U S A, 2010, 107(13), 5839-5844. 2. Qian XP, et al. ACS Med Chem Lett, 2010, 1, 30–34. 3. Lock RB, et al. Pediatr Blood Cancer 2012, 58(6), 916–923. 4. Mayes PA, et al. Int J Cancer, 2013, 132(3), E149-157.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Aging Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Mitochondria-Targeted Compound Library Clinical Compound Library Bioactive Compound Library NO PAINS Compound Library

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Keywords

GSK-923295 1088965-37-0 Apoptosis Cytoskeletal Signaling Kinesin GSK923295 inhibit Inhibitor GSK 923295 inhibitor

 

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