| Identification | Back Directory | [Name]
PhiKan-083 Hydrochloride | [CAS]
880813-36-5 | [Synonyms]
PK083
PhiKan 083
PhiKan-083 Hydrochloride
9-Ethyl-N-methyl-carbazole-3-methanamine
9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-
[(9-Ethyl-9H-carbazol-3-yl)methyl](methyl)amine
9-Ethyl-N-methyl-9H-carbazole-3-methanamine hydrochloride | [Molecular Formula]
C16H18N2 | [MDL Number]
MFCD07366384 | [MOL File]
880813-36-5.mol | [Molecular Weight]
238.33 |
| Chemical Properties | Back Directory | [Boiling point ]
401.0±27.0 °C(Predicted) | [density ]
1.09±0.1 g/cm3(Predicted) | [storage temp. ]
Store at 4°C | [solubility ]
<13.74mg/ml in H2O; <27.48mg/ml in DMSO | [form ]
solid | [pka]
9.71±0.10(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
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]. | [storage]
Store at 4°C | [References]
[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. |
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