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PhiKan 083

In stock
Catalog No.
A4481
p53 stabilizer
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
5mg
$91.00
In stock
10mg
$156.00
In stock
25mg
$364.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

Ki: ≈ 150 M

PhiKan 083 is a critical p53 stabilizing agent by bonding its mutation Y220C

The mutation Y220C of p53 exists a surface cavity that destabilizes the protein by 4 kcal/mol, at a site that is not functional. A p53 stabilizing agent binding it is able to slow rate of thermal denaturation [1].

In vitro: Isothermal titration of PhiKan083 with T-p53C-Y220C exhibited 1:1 stoichiometry and a Kd of 125 ± 10 M. PhiKan083 stabilized T-p53C-Y220C in a concentration-dependent manner. In a simple binding model for PhiKan083 (T-p53C-Y220C at 310 K (37°C)), in the absence of ligand, the protein gave a half-life of 3.8 min, while it increased to 15.7 min at saturating concentrations of PhiKan083. This is a proposed anticancer drug that could be developed for the Y220C mutant using p53 stabilizing agent. The site of mutation in the oncogenic Y220C mutant PhiKan083 binds with reasonable affinity is a druggable target. Interestingly, the site of mutation does not exist in a region of the protein that is functionally important, it will be an excellent target for drug stabilization therapy. This suggests the crystal structure of the complex will be a fresh start for further rounds of drug design and refinement [1].

In vivo: So far, no study in vivo has been conducted.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Boeckler FM, Joerger AC, Jaggi G, Rutherford TJ, Veprintsev DB, Fersht AR.  Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29; 105(30):10360-5.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at 4°C
M.Wt274.79
Cas No.880813-36-5
FormulaC16H18N2.HCl
Solubility<13.74mg/ml in H2O; <27.48mg/ml in DMSO
Chemical Name1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride
SDFDownload SDF
Canonical SMILESCNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

PhiKan 083