NVP-231

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Chemical Structure| 362003-83-6 同义名 : -
CAS号 : 362003-83-6
货号 : A149574
分子式 : C25H25N3O2S
纯度 : 98+%
分子量 : 431.55
MDL号 : MFCD01988824
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(92.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.59mL

2.32mL

1.16mL

23.17mL

4.63mL

2.32mL
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