|N-(2-苯甲酰胺基苯并噻唑-6-基)金刚烷-1-甲酰胺|CsnPharm

CAS No.: 362003-83-6

N-(2-Benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide Catalog No. CSN18240

Synonyms: NVP-231

NVP-231 is a potent, selective and reversible ceramide kinase (CerK) inhibitor with IC50 of 12 nM.

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技术信息

生物活性

描述Ceramide kinase (CerK), which belongs to the diacylglycerol kinase superfamily, produces the bioactive lipid ceramide-1-phosphate (C1P) and appears as a key enzyme for controlling ceramide levels. NVP-231 is a potent, specific, and reversible CerK inhibitor that competitively inhibits binding of ceramide to CerK with an IC₅₀ value of 12 nM. At 10 nM, NVP-231 inhibited C1P formation by 50%; at 100 nM, NVP-231 achieved complete inhibition in human CerK-overexpressing COS-cells. Similar drop could also be found in mouse peritoneal macrophages and mouse bone marrow-derived mast cells^[3]. When treating either MCF-7 or NCI-H358 cells with NVP-231 for 48h, viability was concentration-dependently reduced with an IC₅₀ of about 1 μM in MCF-7 cells and 500 nM in NCI-H358 cells. Further, 1 μM NVP-231 caused a 60–70% reduction of DNA synthesis after 72h in both cell lines. Moreover, cell cycle analysis revealed that NVP-231 (24h treatment with increasing concentrations) decreased the number of cells in S phase and induced M phase arrest with an increased mitotic index^[4].
参考文献

[1] Pastukhov O, Schwalm S, et al. The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death. Br J Pharmacol. 2014 Dec;171(24):5829-44.
[2] Graf C, Klumpp M, et al. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32.
[3] Graf C, Klumpp M, Habig M, Rovina P, Billich A, Baumruker T, Oberhauser B, Bornancin F. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32
[4] Pastukhov O, Schwalm S, Zangemeister-Wittke U, et al. The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death. Br J Pharmacol. 2014 Dec;171(24):5829-44

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3172 mL
- 11.5861 mL
- 23.1723 mL
- 5 mM
- 0.4634 mL
- 2.3172 mL
- 4.6345 mL
- 10 mM
- 0.2317 mL
- 1.1586 mL
- 2.3172 mL

技术信息

CAS号

362003-83-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H25N3O2S

运输

蓝冰

分子量

431.55

别名

NVP-231

溶解度

DMSO	86.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	8.0 mg/mL (18.5 mM)

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N-(2-Benzamidobenzo[d]thiazol-6-yl)adamantane-1-carboxamide Catalog No. CSN18240

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