880813-36-5
880813-36-5 结构式
基本信息
PhiKan 083
PhiKan-083 Hydrochloride
9-Ethyl-N-methyl-carbazole-3-methanamine
9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-
[(9-Ethyl-9H-carbazol-3-yl)methyl](methyl)amine
9-Ethyl-N-methyl-9H-carbazole-3-methanamine hydrochloride
物理化学性质
常见问题列表
Kd: 167 μM (p53-Y220C), 150 μM (p53 Y220C , in Ln229 cells)
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, shows a relative binding affinity (K
d
) of 150 μM for p53
Y220C
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
wt
, p53
Y220C
, p53
G245S
, p53
R282W
).
Cell Viability Assay
| 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. |