NVP-231
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- CAS号:
- 362003-83-6
- 英文名:
- N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide
- 英文别名:
- NVP 231;CS-1722;NVP-231;NVP231;NVP-231;NVP 231;NVP231;N-(2-Benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide;adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide;(3r,5r,7r)-N-(2-benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide;N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide;NVP231,inhibit,mcf-7,cancer,cerk,Apoptosis,NVP 231,Inhibitor,NCI-H358,NVP-231;Tricyclo[3.3.1.13,7]decane-1-carboxamide, N-[2-(benzoylamino)-6-benzothiazolyl]-
- 中文名:
- NVP-231
- 中文别名:
- 化合物NVP 231;CERK抑制剂(NVP 231);N-(2-苯甲酰胺基苯并噻唑-6-基)金刚烷-1-甲酰胺
- CBNumber:
- CB42518895
- 分子式:
- C25H25N3O2S
- 分子量:
- 431.55
- MOL File:
- 362003-83-6.mol
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NVP-231化学性质
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熔点:
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246-248 °C(Solv: isopropanol (67-63-0); water (7732-18-5))
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密度:
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1.398±0.06 g/cm3(Predicted)
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储存条件:
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Store at +4°C
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溶解度:
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DMSO: >10mg/mL
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酸度系数(pKa):
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9.09±0.70(Predicted)
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形态:
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powder
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颜色:
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white to off-white
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稳定性:
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Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
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InChIKey:
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MVSSJPGNLQPWSW-UHFFFAOYSA-N
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SMILES:
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C12(C(NC3C=C4SC(NC(=O)C5=CC=CC=C5)=NC4=CC=3)=O)CC3CC(CC(C3)C1)C2
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NVP-231性质、用途与生产工艺
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。
| Target | Value |
CreK
(Cell-free assay)
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12 nM
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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
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Cell Line:
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MCF-7 cells; NCI-H358 cells
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Concentration:
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0 nM, 10 nM, 100 nM, 300 nM, 500 nM, 1000 nM
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Incubation Time:
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48 hours
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Result:
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Reduced MCF-7 cells and NCI-H358 cells in a concentration manner.
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Apoptosis Analysis
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Cell Line:
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MCF-7 cells; NCI-H358 cells
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Concentration:
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1000 nM
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Incubation Time:
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24-72 hours
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Result:
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Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells.
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Western Blot Analysis
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Cell Line:
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MCF-7 cells; NCI-H358 cells
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Concentration:
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0 nM, 100 nM, 300 nM, 500 nM
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Incubation Time:
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24 hours
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Result:
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Decreased p-cyclin B1, p-CDK1 as a concentration manner.
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NVP-231
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-13945 | NVP 231 | | 1 mg | 171元 |
| 2024/04/30 | HY-13945 | NVP 231 | | 5 mg | 343元 |
362003-83-6, NVP-231 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 抑制剂
- 小分子抑制剂
- N-(2-苯甲酰胺基苯并噻唑-6-基)金刚烷-1-甲酰胺
- 化合物NVP 231
- CERK抑制剂(NVP 231)
- 362003-83-6
- (3r,5r,7r)-N-(2-benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide
- N-(2-Benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide
- NVP231,inhibit,mcf-7,cancer,cerk,Apoptosis,NVP 231,Inhibitor,NCI-H358,NVP-231
- Tricyclo[3.3.1.13,7]decane-1-carboxamide, N-[2-(benzoylamino)-6-benzothiazolyl]-
- NVP-231;NVP 231;NVP231
- CS-1722
- NVP-231;NVP231
- NVP 231
- N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide
- adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide