[CAS NO. 880813-36-5] PhiKan 083
PRODUCTS SPECIFICATIONS [880813-36-5]
DESCRIPTION [880813-36-5]
Overview
| MDL | MFCD07366384 |
|---|---|
| Molecular Weight | 238.33 |
| Molecular Formula | C16H18N2 |
| SMILES | CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3 |
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
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 419.59 mM ; Need ultrasonic)
Ethanol : 100 mg/mL ( 419.59 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.1959 mL | 20.9793 mL | 41.9586 mL |
| 5 mM | 0.8392 mL | 4.1959 mL | 8.3917 mL |
| 10 mM | 0.4196 mL | 2.0979 mL | 4.1959 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.