NVP-231

生物活性靶点体外研究 NVP-231 试剂级价格

NVP-231

CAS号:362003-83-6
英文名:N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide
中文名:NVP-231
CBNumber:CB42518895
分子式:C25H25N3O2S
分子量:431.55
MOL File:362003-83-6.mol

NVP-231化学性质

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
酸度系数(pKa) :9.09±0.70(Predicted)
形态 :powder
颜色 :white to off-white
稳定性 :Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
InChIKey :MVSSJPGNLQPWSW-UHFFFAOYSA-N
SMILES :C12(C(NC3C=C4SC(NC(=O)C5=CC=CC=C5)=NC4=CC=3)=O)CC3CC(CC(C3)C1)C2

安全信息

WGK Germany :nwg

NVP-231性质、用途与生产工艺

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

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.