1050480-30-2
| 中文名称 | 1050480-30-2 |
|---|---|
| 中文同义词 | 化合物 T16523;1-(9-乙基-9H-咔唑-3-基)-N-甲基甲胺盐酸盐;PHIKAN 083,P53稳定剂 |
| 英文名称 | PhiKan 083 hydrochloride |
| 英文同义词 | PhiKan083 hydrochloride >=98% (HPLC);1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride |
| CAS号 | 1050480-30-2 |
| 分子式 | C16H19ClN2 |
| 分子量 | 274.79 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1050480-30-2.mol |
| 结构式 |  |
1050480-30-2 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 在水中溶解度为 50 mM，在 DMSO 中溶解度为 100 mM |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
| 水溶解性 | Water: 2 mg/mL (7.28 mM and warming) |
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. |