PhiKan 083 hydrochloride

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].

Product Specifications

CAS Number

[1050480-30-2]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PhiKan_083_hydrochloride.html

Purity

99.27

Solubility

DMSO : 62.5 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 2 mg/mL (ultrasonic; warming)

Smiles

CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.[H]Cl

Molecular Formula

C16H19ClN2

Molecular Weight

274.79

Precautions

H315, H319

References & Citations

[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.