PhiKan-083

Research use only, not for human use.

A small-molecule stabilizer of p53 mutant Y220C with Kd of 150 uM.

A small-molecule stabilizer of p53 mutant Y220C with Kd of 150 uM; binds with high affinity to a crevice created by the Y220C mutation in p53 and stabilizes the mutant protein.

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells.PhiKan 083 slows down its thermal denaturation rate.PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells. PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W). Cell Viability Assay Cell Line:Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells Concentration:125 μM Incubation Time:48 hours Result:Caused ～70 ± 5% reduction in cell viability of variants of Ln229 cells.

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PK-083

Apoptosis

MDM2-p53

MDM2-p53

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1050480-30-2

274.792

C16H18N2.HCl

>98% (HPLC)

H2O : 2 mg/mL7.28 mM

CCN1C2=C(C=C(C=C2)CNC)C3=CC=CC=C31.Cl

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

(-20℃)

With Ice Pack

≥ 2 years