Eg5-I
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 127 and 190 nM for enzyme and cell, respectively
Eg5-I is a potent inhibitor of Eg5.
The kinesin-like spindle protein Eg5, also known as KSP and Kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.
In vitro: Previous study found that the interphase microtubule morphology was normal after the treatment of Eg5-I, whereas spindle morphology mirrored that of the parent compound. Eg5-I was tested for inhibitory activity against a selected panel of mitotic kinesins with no measurable inhibition detected. To determine whether Eg5-I had a similar effect on KSP dynamics, cells were treated with Eg5-I and probed for KSP localization with anti-KSP antibodies. Eg5-I showed a dose-dependent depletion of KSP from the spindle, with a 1.63-fold increase in clearance of KSP over its parent compound, consistent with the biochemical-and cell-based assays. Eg5-I blocked bipolar spindle formation, whereas the parent compound was weakly active. Eg5-I was also evaluated for anti-proliferative activity against the NCI60 tumor panel and the growth inhibitory concentration anged from 10 nM to 3 μM across the panel, respectively [1].
In vivo: Up to now, there is no animal in vivo data reported for Eg5-I.
Clinical trial: So far, no clinical study has been conducted for Eg5-I.
Reference:
[1] Rodriguez, D. ,Ramesh, C.,Henson, L.H., et al. Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity. Bioorganic & Medicinal Chemistry 19(18), 5446-5453 (2011).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 379.5 |
Cas No. | 1338701-15-7 |
Formula | C23H25NO2S |
Solubility | ≤1mg/ml in ethanol;25mg/ml in DMSO;5mg/ml in dimethyl formamide |
Chemical Name | (2R)-2-amino-3-[[(4-methoxyphenyl)diphenylmethyl]thio]-1-propanol |
SDF | Download SDF |
Canonical SMILES | OC[C@@H](N)CSC(C1=CC=C(OC)C=C1)(C2=CC=CC=C2)C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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