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Submit ReviewGSK 923295A
Description: Potent and selective centromere associated protein E (CENP-E) allosteric inhibitor
Chemical Name: 3-Chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)benzamide
Purity: ≥97% (HPLC)
Biological Activity for GSK 923295A
GSK 923295A is a potent and selective centromere associated protein E (CENP-E) allosteric inhibitor (IC50 = 22 nM); does not compete with ATP. Exhibits selectivity over a panel of other kinesins (<25% inhibition at 50 μM). Inhibits tumor cell growth in vitro. Induces mitotic arrest and regression of human tumor xenografts in vivo.
Technical Data for GSK 923295A
| M. Wt | 592.13 |
| Formula | C32H38ClN5O4 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1088965-37-0 |
| PubChem ID | 46898058 |
| InChI Key | WHMXDBPHBVLYRC-OFVILXPXSA-N |
| Smiles | CC(OC1=C(C=C(C(N[C@@H](CC2=CC=C(C3=CN4C=CC=C(C4=N3)[C@@H](O)C)C=C2)CNC(CN(C)C)=O)=O)C=C1)Cl)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for GSK 923295A
References for GSK 923295A
References are publications that support the biological activity of the product.
Qian et al (2010) Discovery of the first potent and selective inhibitor of centromere-associated protein E: GSK923295. ACS Med.Chem.Lett. 1 30 PMID: 24900171
Wood et al (2010) Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc.Natl.Acad.Sci.U.S.A. 107 5839 PMID: 20167803
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Keywords: GSK 923295A, GSK 923295A supplier, GSK923295A, ATPase, Potent, selective, centromere, associated, protein, E, CENP-E, allosteric, inhibitors, inhibits, mitotic, kinesin, mitosis, Kinesin, 6837, Tocris Bioscience
Citations for GSK 923295A
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Cell Cycle and DNA Damage Research Product Guide
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