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
- 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
- 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.
- 更新日期：2025/02/08
- 产品编号：HY-13945
- 产品名称：NVP 231
- CAS编号：362003-83-6
- 包装：1 mg
- 价格：171元
- 更新日期：2025/02/08
- 产品编号：HY-13945
- 产品名称：NVP 231
- CAS编号：362003-83-6
- 包装：5 mg
- 价格：343元
- 公司名称：A.J Chemicals
- 联系电话：--
- 电子邮件：sales@ajchem.in
- 国家：印度
- 产品数：6100
- 优势度：58
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
- N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐 (1:1) BI 2536 阿卡替尼 瑞卡帕布（AG-014699） NVP-HDM201 BAW2881 6-[[2-[[2-(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethyl]amino]ethyl]amino-3-pyridinecarbononitriledihydrochloride NVP-BSK805 dihydrochloride NVP-BGT226 TAE226 (NVP-TAE226) 4-(2,6-二氯苯甲酰基氨基)-1H-吡唑-3-羧酸 N-[1-(甲基磺酰基)哌啶-4-基]酰胺 NVP-TAE684 NVP-BEZ235
