Name: GSK-923295
Price: 392.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK923295 is a specific inhibitor of CENP-E kinesin motor with IC50 value of 3.2 nM [1].
    Centromere-associated protein E (CENP-E) is a mitotic kinesin, which is the connect of mitosis process with the mitotic checkpoint signaling. It Interacts with spindle microtubules and contribute to the chromosome alignment, and thus it regulates the cell-cycle transition from metaphase to anaphase.
    When asynchronous cultured cells were exposed to GSK923295, the penetrant cell-cycle delay in mitosis was observed, which accompanied with morphological changes similar to RNAi-mediated knockdown of CENP-E mRNA. It indicated a significant inhibition of CENP-E by GSK923295. In the presence of GSK9232195, CENP-E microtubule (MT)-stimulated ATPase showed a dramatic slowing of release of ADP and Pi, where the ATP-bound form was stabilized and the activity of CENP-E was inhibited. This observation suggested GSK923295 inhibited CENP-E via the suppression of MT-stimulated ATPase [1].
    In mouse model, mice bearing xenografts of the Colo205 colon tumor cell line were administered with GSK923295 of 125 mg/kg. The result showed GSK923295-induced cell-cycle changes of tumor cells and increased scattered apoptosis body. Additionally, long-term study via measuring tumor volume revealed significant antitumor activity of GSK923295, in a manner of dose-dependent [1].
- Properties
  - Alternative Name
    
    GSK 923295;GSK923295; 3-chloro-N-[(2S)-1-[[2-(dimethylamino)acetyl]amino]-3-[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]propan-2-yl]-4-propan-2-yloxybenzamide
    
    CAS Number
    
    1088965-37-0
    
    Molecular Formula
    
    C32H38ClN5O4
    
    Molecular Weight
    
    592.14
    
    Appearance
    
    A solid
    
    Purity
    
    99.70%
    
    Solubility
    
    ≥29.6 mg/mL in DMSO; insoluble in H2O; ≥14.87 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mikito Owa, Brian Dynlacht. "A non-canonical function for Centromereassociated protein-E controls centrosome integrity and orientation of cell division." Commun Biol. 2021 Mar 19;4(1):358. PMID: 33742057
    2. Amin MA, McKenney RJ, et al. "Antagonism between the dynein and Ndc80 complexes at kinetochores controls the stability of kinetochore-microtubule attachments during mitosis." J Biol Chem. 2018 Apr 20;293(16):5755-5765. PMID:29475948

GSK-923295

GSK-923295

Background

We Also Recommend

Guanfacine hydrochloride

GW-1100

GW1929