PhiKan 083 是一种咔唑衍生物，可以稳定 p53 的突变体 Y220C，K_d 值为 167 μM。PhiKan 083 可用于癌症研究。

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K d of 167 μM. PhiKan 083 can be used for cancer research.

Solid

Kd: 167 μM (p53-Y220C), 150 μM (p53, in Ln229 cells)

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 p53 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 (p53, p53, p53, p53). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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]. Paulmuruga

In Vitro: DMSO : 100 mg/mL (419.59 mM; Need ultrasonic)Ethanol : 100 mg/mL (419.59 mM; Need ultrasonic)配制储备液