產品屬性：
產品名稱 | PhiKan 083 hydrochloride |
規格 | 5mg、10mg、25mg、50mg、100mg |
貨號 | EY-01Y12389 |
Cas No.: 1050480-30-2
別名: N/A
化學名: N/A
分子式: C16H19ClN2
分子量: 274.79
溶解度: H2O: 2 mg/mL (7.28 mM and warming)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], and a relative binding affinity (Kd) of 150 μM in Ln229 cells[3].Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3].PhiKan 083 slows down its thermal denaturation rate[2].PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells[3]. PhiKan 083 (100 μM) in conbination with doxorubicin (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W)[3].Cell Viability Assay[1] Cell Line:Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells[1]. Boeckler FM, et al. 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.
[2]. Rauf SM, et al. Effect of Y220C mutation on p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013 Jan;32(1):68-74.
[3]. Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511.
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