PhiKan-083 Hydrochloride Struktur

PhiKan-083 Hydrochloride

Bezeichnung:PhiKan-083 Hydrochloride

CAS-Nr880813-36-5

Englisch Name:PhiKan-083 Hydrochloride

CBNumberCB02652533

SummenformelC16H18N2

Molgewicht238.33

MOL-Datei880813-36-5.mol

PhiKan-083 Hydrochloride physikalisch-chemischer Eigenschaften

Siedepunkt	401.0±27.0 °C(Predicted)
Dichte	1.09±0.1 g/cm3(Predicted)
storage temp.	Store at 4°C
Löslichkeit	<13.74mg/ml in H2O; <27.48mg/ml in DMSO
Aggregatzustand	solid
pka	9.71±0.10(Predicted)
Farbe	White

Gefahreninformationscode (GHS)

PhiKan-083 Hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
PhiKan-083 is a p53 stabilizing agent. PhiKan-083 preferentially binds mutated (Y220C) p53 over wild-type p53 at a site distinct from functional DNA/protein interaction regions. PhiKan-083 slows rate of thermal denaturation of p53-Y220C.
Biologische Aktivität
ki: ≈ 150 mphikan 083 is a critical p53 stabilizing agent by bonding its mutation y220cthe 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].
Einzelnachweise
[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.

PhiKan-083 Hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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