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

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhiKan 083 hydrochlorideCat. No.: HY-108637ACAS No.: 1050480-30-2分式: CHClN分量: 274.79作靶點(diǎn): MDM-2/p53作通路: Apoptosis儲(chǔ)存式: Powder -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) H2O : 2 mg/mL (7.28 mM; Need ultraso

2、nic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.6391 mL 18.1957 mL 36.3914 mL5 mM 0.7278 mL 3.6391 mL 7.2783 mL10 mM - - -請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 PhiKan 083 hydrochloride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(duì)親和 (Kd) 為 150

3、 M 3；PhiKan 083 可于癌癥研究 1。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 cavity 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 Ln22

4、9 cells 3.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEPhiKan 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 083 (100 M) in conbination with doxorubicin (1 M) enhances the pro-apoptotic activit

5、y 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: 48 hoursResult: Caused -70 5% reduction in cell viability of variants of Ln229 cel

6、ls.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 p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013Jan;32(1)

7、: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 use