CAS NO: | 880813-36-5 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Cas No. | 880813-36-5 |
化学名 | 1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride |
Canonical SMILES | CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.Cl |
分子式 | C16H18N2.HCl |
分子量 | 274.79 |
溶解度 | <13.74mg/ml in Water;<27.48mg/ml in DMSO |
储存条件 | Store at 4℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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℃)), 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: |