362003-83-6

中文名称 NVP-231

英文名称 N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide

CAS 362003-83-6

分子式 C25H25N3O2S

分子量 431.55

MOL 文件 362003-83-6.mol

更新日期 2023/03/20 15:41:25

362003-83-6 结构式

基本信息物理化学性质安全数据图谱信息 NVP-231价格(试剂级) 常见问题列表

基本信息

中文别名

CERK抑制剂(NVP 231)

英文别名

NVP 231
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]-

所属类别

生物化工：激动剂抑制剂

物理化学性质

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

溶解度二甲基亚砜：>10mg/mL

酸度系数(pKa)9.09±0.70(Predicted)

形态粉末

颜色白色至灰白色

稳定性可在-20°C下的DMSO溶液中保存长达1个月。

InChIKeyMVSSJPGNLQPWSW-UHFFFAOYSA-N

SMILESC12(C(NC3C=C4SC(NC(=O)C5=CC=CC=C5)=NC4=CC=3)=O)CC3CC(CC(C3)C1)C2

安全数据

WGK Germanynwg

图谱信息

NVP-231(362003-83-6)核磁图(¹HNMR)

NVP-231价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2025/02/08	HY-13945	NVP 231	362003-83-6	1 mg	171元
2025/02/08	HY-13945	NVP 231	362003-83-6	5 mg	343元
2025/02/08	HY-13945	NVP-231 NVP 231	362003-83-6	10mg	550元

常见问题列表

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.