性能参数

产品名称

PhiKan 083

规格

0mg 50mg

货号

GOY-Y3136

 含量

>98.00%

CAS

880813-36-5

别名

化学名

1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride

分子式

C16H18N2.HCl

分子量

分子量 274.79

溶解度

<13.74mg/ml in H2O; <27.48mg/ml in DMSO

储存条件

Store at 4°C

General tips

用途

仅供科研

价格

电询

详细内容

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.

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BRD71

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