362003-83-6
362003-83-6 结构式
基本信息
CS-1722
NVP-231
NVP231
NVP-231
NVP 231
NVP231
adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide
N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide
Tricyclo[3.3.1.13,7]decane-1-carboxamide, N-[2-(benzoylamino)-6-benzothiazolyl]-
物理化学性质
常见问题列表
| Target | Value |
|
CreK
(Cell-free assay) | 12 nM |
NVP-231 (0-500 nM; 24 hours) gradually reduces the cellular CerK activity, as measured by NBD-C1P formation, demonstrating that NVP-231 active in transfected cells. The IC 50 for CerK in this cellular system is 59.70 ± 12 nM. NVP-231 (0-1000 nM; 48 hours) decreases cell viability as a dose-dependent manner. This compound shows IC 50 values of 1 μM in MCF-7 cells and 500 nM in NCI-H358 cells. NVP-231 (1 μM; 24-72 hours) induces caspase-3 and caspase-9 cleavage in both cell lines. However, the highest caspase-3 and caspase-9 cleavage and activation occurred at 24 hours in MCF-7 cells, then decreases again. In NCI-H358 cells, caspase-3 and caspase-9 cleavage occurrs continuously over 72 hours. NVP-231 (0-500 nM; 24 hours) causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. The total CDK1 expression also declined upon CerK inhibition.
Cell Viability Assay
| Cell Line: | MCF-7 cells; NCI-H358 cells |
| Concentration: | 0 nM, 10 nM, 100 nM, 300 nM, 500 nM, 1000 nM |
| Incubation Time: | 48 hours |
| Result: | Reduced MCF-7 cells and NCI-H358 cells in a concentration manner. |
Apoptosis Analysis
| Cell Line: | MCF-7 cells; NCI-H358 cells |
| Concentration: | 1000 nM |
| Incubation Time: | 24-72 hours |
| Result: | Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells. |
Western Blot Analysis
| Cell Line: | MCF-7 cells; NCI-H358 cells |
| Concentration: | 0 nM, 100 nM, 300 nM, 500 nM |
| Incubation Time: | 24 hours |
| Result: | Decreased p-cyclin B1, p-CDK1 as a concentration manner. |