GSK-923295

SKU: orb1306666

Description

GSK923295 is a potent and selective allosteric inhibitor of the mitotic kinesin CENP-E, with a reported inhibition constant (Ki) of 3.2 nM. It is a valuable chemical probe for studying mitosis, aneuploidy, and has been utilized in both in vitro biochemical assays and in vivo tumor xenograft models to investigate antimitotic therapies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1088965-37-0
• MW: 592.13
• Purity: 99.71%
• Formula: C₃₂H₃₈ClN₅O₄
• SMILES: CC(C)Oc1ccc(cc1Cl)C(=O)N[C@H](CNC(=O)CN(C)C)Cc1ccc(cc1)-c1cn2cccc([C@H](C)O)c2n1
• Target: Kinesin,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (4.22 mM);DMSO:93 mg/mL (157.06 mM);Ethanol:93 mg/mL (157.06 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  CENP-E:3.2 nM(Ki)
• In Vivo:
  In cancer cell lines, GSK923295 exhibits broad-spectrum antitumor activity, demonstrating effectiveness against SW48 (IC50=17.2 nM), RKO (BRAF mutant) (IC50=55.6 nM), SW620 (KRAS mutant) (IC50=42 nM), and HCT116 (KRAS mutant) (IC50=51.9 nM). Additionally, in human neuroblastoma cell lines, GSK923295 shows an average growth inhibition (IC50) of 41 nM.
• In Vitro:
  In various solid tumor models, including Ewing's sarcoma, sarcoma, and transplanted rhabdomyosarcoma tumors, GSK923295 consistently demonstrates significant antitumor activity. In Colo205 transplanted tumor models, GSK923295 (125 mg/kg) effectively inhibits tumor growth, resulting in a marked increase in mitosis and free apoptotic bodies.
• 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)

Storage & Handling

• Storage: store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CENP-E, Apoptosis, Inhibitor, GSK 923295, GSK923295, GSK-923295, Kinesin, inhibit

Compound Identifiers

PubChem CID

46898058