NVP-231
中文名称:
NVP-231
中文同义词:
CERK抑制剂(NVP 231)
英文名称:
N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide
英文同义词:
adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide;N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide;NVP 231;NVP-231;NVP231;CS-1722;NVP-231;NVP 231;NVP231;Tricyclo[3.3.1.13,7]decane-1-carboxamide, N-[2-(benzoylamino)-6-benzothiazolyl]-
CAS号:
362003-83-6
分子式:
C25H25N3O2S
分子量:
431.55
EINECS号:
相关类别:
细胞生物学试剂;小分子抑制剂;抑制剂;小分子抑制剂，天然产物;Inhibitors
Mol文件:
362003-83-6.mol
熔点
246-248 °C(Solv: isopropanol (67-63-0); water (7732-18-5))
密度
1.398±0.06 g/cm3(Predicted)
储存条件
Store at +4°C
溶解度
DMSO: >10mg/mL
形态
powder
酸度系数(pKa)
9.09±0.70(Predicted)
颜色
white to off-white
生物活性
NVP 231是新型CerK抑制剂，在体外抑制重组CerK的催化活性，IC50为12 nM。
靶点
Target Value
CreK
(Cell-free assay) 12 nM
Target
Value
CreK
(Cell-free assay)
12 nM
体外研究
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.
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.
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.
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.
WGK Germany
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