A cell-permeable

Ispinesib – 5 mg

Brand:
Cayman
CAS:
336113-53-2
Storage:
-20
UN-No:
Non-Hazardous - /

The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells.{22151} Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM) with >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins.{29618,29621} It induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death (GI50s = 22-82 nM in colon, pancreas, prostrate, and lung cancer cells in vitro).{22151} At 10 mg/kg, ispinesib produces tumor regression of breast cancer cell xenografts in mice.{29619} It has also been used to halt the growth of treatment-resistant glioblastoma tumor-initiating cells, to prevent tumor initiation and self-renewal of a cancer stem cell population (EC50 = 1.15 nM), and to reduce glioma cell invasion.{29620}  

 

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Description

A cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM) with >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins,

Formal name: N-​(3-​aminopropyl)​-​N-​[(1R)​-​1-​[7-​chloro-​3,​4-​dihydro-​4-​oxo-​3-​(phenylmethyl)​-​2-​quinazolinyl]​-​2-​methylpropyl]​-​4-​methyl-benzamide

Synonyms:  SB-715992

Molecular weight: 517.1

CAS: 336113-53-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cancer Stem Cell Research|Proliferation||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cytoskeleton & Motor Proteins

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