5.30390
Mitosis Inhibitor, AK301
Synonym(s):
Mitosis Inhibitor, AK301, TNF sensitizing agent
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About This Item
Empirical Formula (Hill Notation):
C19H21ClN2O2
Molecular Weight:
344.84
UNSPSC Code:
12352200
storage temp.
2-8°C
assay
≥98% (HPLC)
form
solid
potency
115 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 25 mg/mL
Quality Level
General description
A cell permeable piperazine derivative that induces irreversible mitotic arrest in colon cancer cells (IC50 = 115 nM in HT29 cells) and increases their sensitivity to TNF-induced apoptosis (EC50 = 172 nM). Also shown to enhance FasL and TRAIL-induced caspase-3 activity in colon cancer cells. Binds to the chochicine-binding domain on b-tubulin with high affinity, although in a different orientation than cholchicine, and reduces tubulin polymerization with formation of multiple microtubule organizing centers with Aurora kinase A and g-tubulin. Induces G2/M arrest in both HT29 colon cancer cells and WI38 lung fibroblasts, however, this effect is more pronounced in cancer cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
tubulin
tubulin
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chopra, A. S., et al. 2013. J. Bio. Chem.289, 2978.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Certificates of Analysis (COA)
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