[CAS NO. 1050480-30-2] PhiKan 083 hydrochloride
PRODUCTS SPECIFICATIONS [1050480-30-2]
DESCRIPTION [1050480-30-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 274.79 |
| Molecular Formula | C16H19ClN2 |
| SMILES | CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.[H]Cl |
Summary
In Vitro
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
[1]
, shows a relative binding affinity (K
d
) of 150 μM for p53
Y220C
in Ln229 cells
[3]
.
PhiKan 083 slows down its thermal denaturation rate
[2]
.
PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells
[3]
.
PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53
wt
, p53
Y220C
, p53
G245S
, p53
R282W
)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 62.5 mg/mL ( 227.45 mM ; ultrasonic and warming and heat to 60°C)
H 2 O : 2 mg/mL ( 7.28 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.6391 mL | 18.1957 mL | 36.3914 mL |
| 5 mM | 0.7278 mL | 3.6391 mL | 7.2783 mL |
| 10 mM | 0.3639 mL | 1.8196 mL | 3.6391 mL |
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.