SML3220
GSK923295
≥95% (HPLC)
Synonym(s):
3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide, GSK 923295, GSK 923295A
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About This Item
Empirical Formula (Hill Notation):
C32H38ClN5O4
CAS Number:
Molecular Weight:
592.13
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
Clc1c(ccc(c1)C(=O)N[C@H](CNC(=O)CN(C)C)Cc2ccc(cc2)c3nc4[n](c3)C=CC=C4[C@@H](O)C)OC(C)C
InChI key
WHMXDBPHBVLYRC-OFVILXPXSA-N
Biochem/physiol Actions
GSK923295 is an allosteric inhibitor of CENP-E kinesin motor ATPase activity. It inhibits release of inorganic phosphate and stabilizes CENP-E motor domain interaction with microtubules, which causes failure of metaphase chromosome alignment and induces mitotic arrest. GSK923295 induces tumor cell apoptosis and tumor regression
Selective and potent allosteric inhibitor of CENP-E kinesin motor ATPase activity
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295
ACS Medicinal Chemistry Letters, 1(1), 30-34 (2010)
Zhen-Yu She et al.
Cell death discovery, 6, 25-25 (2020-05-01)
Kinesin-7 CENP-E is an essential kinetochore motor required for chromosome alignment and congression. However, the specific functions of CENP-E in the spermatogenic cells during spermatogenesis remain unknown. In this study, we find that CENP-E proteins are expressed in the spermatogonia
Rudolf Pisa et al.
Cell chemical biology, 27(7), 850-857 (2020-05-23)
Aberrant chromosome numbers in cancer cells may impose distinct constraints on the emergence of drug resistance-a major factor limiting the long-term efficacy of molecularly targeted therapeutics. However, for most anticancer drugs we lack analyses of drug-resistance mechanisms in cells with
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