PhiKan 083
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: ≈ 150 μM
PhiKan 083是一种关键的p53稳定剂,结合其突变Y220C。
P53的突变Y220C存在一种表面腔,在非功能位点破坏蛋白质(4 kcal/mol)。P53稳定剂与其结合能够减缓热变性速率[1]。
体外:用T-p53C-Y220C进行 PhiKan083等温滴定表现出1:1的化学计量和125 ± 10 μM的Kd值。PhiKan083浓度依赖性地稳定T-p53C-Y220C。PhiKan083(T-p53C-Y220C 在310 K(37℃))的简单结合模型中,在不存在配体的情况下,蛋白质半衰期为3.8分钟,而在PhiKan083饱和浓度下增加至15.7分钟。它被认为是一种使用p53稳定剂为Y220C突变开发的抗癌药物。致癌Y220C突变中PhiKan083具有适当结合亲和力的突变位点是一个成药靶点。有意义的是,突变位点不存在于具有重要功能的蛋白区域,这将是药物稳定治疗的优异靶点。这表明,该复合物的晶体结构将是未来几轮药物设计和改进的一个新起点[1]。
体内:目前尚未进行体内研究。
临床试验:目前尚未进行临床研究。
参考文献:
[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.
Physical Appearance | White solid |
Storage | Store at 4°C |
M.Wt | 274.79 |
Cas No. | 880813-36-5 |
Formula | C16H18N2·HCl |
Solubility | <13.74mg/ml in H2O; <27.48mg/ml in DMSO |
Chemical Name | 1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride |
SDF | Download SDF |
Canonical SMILES | CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |