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, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.

Product information

CAS Number: 1050480-30-2

Molecular Weight: 274.79

Formula: C16H19ClN2

Chemical Name: [(9-ethyl-9H-carbazol-3-yl)methyl](methyl)amine hydrochloride

Smiles: Cl.CCN1C2=CC=C(CNC)C=C2C2=CC=CC=C12

InChiKey: IXWVUPURFWFRNE-UHFFFAOYSA-N

InChi: InChI=1S/C16H18N2.ClH/c1-3-18-15-7-5-4-6-13(15)14-10-12(11-17-2)8-9-16(14)18;/h4-10,17H,3,11H2,1-2H3;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 2 mg/mL (7.28 mM; Need ultrasonic and warming)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], 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).

References:

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.

Products are for research use only. Not for human use.