PhiKan-083-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhiKan 083Cat. No.: HY-108637CAS No.: 880813-36-5分式: CHN分量: 238.33作靶點(diǎn): MDM-2/p53作通路: Apoptosis儲存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 130 mg/mL (545.46 mM; Need ultrasonic)H2O :

2、40% PEG300 5% Tween-80 45% salineSolubility: 2.17 mg/mL (9.11 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (9.11 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.17

3、mg/mL (9.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 PhiKan 083種咔唑衍物，可以穩(wěn)定 p53 的突變體 Y220C，Kd 值為 167 M 1，在 Ln229 細(xì)胞中，相對親和 (Kd) 為 150 M；PhiKan 083 可于癌癥研究 1 3。IC50 & Target Kd: 167 M (p53-Y220C) 1, 150 M (p53Y220C, in Ln229 cells) 3體外研究 PhiKan 083 is a carbazole derivative, which binds to the surface c

4、avity and stabilizes Y220C (a p53 mutant),with a Kd of 167 M 1, shows a relative binding affinity (Kd) of 150 M for p53Y220C in Ln229 cells 3.PhiKan 083 slows down its thermal denaturation rate 2.PhiKan 083 (125 M, 48 hours) reduces the cell viability of engineered variants of Ln229 cells 3.PhiKan 0

5、83 (100 M) in conbination with doxorubicin (1 M) enhances the pro-apoptotic activity in allvariants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W) 3.Cell Viability Assay 1Cell Line: Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cellsConcentration: 125 MIncubation Time:

6、 48 hoursResult: Caused -70 5% reduction in cell viability of variants of Ln229 cells.REFERENCES1. 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 Jul29;105(30):10360-5.2. Rauf SM, et al. Effect of Y220C mutation on p5

7、3 and its rescue mechanism: a computer chemistry approach. Protein J. 2013Jan;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 andits downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511.McePdfHeightCaution: Product has not been fully validated for medical applications.For research