货号	规格	价格	上海	北京	珠海	重庆	武汉
S85091-5mg	99.06%	￥100.00 S85091-5mg ￥100.00 现货	7 7	-	-	-	-
S85091-10mg	99.06%	￥130.00 S85091-10mg ￥130.00 现货	6 6	-	-	-	-
S85091-25mg	99.06%	￥200.00 S85091-25mg ￥200.00 现货	6 6	-	-	-	-
S85091-100mg	≥99%	￥360.00 S85091-100mg ￥360.00 2-3天	0 货期：2-3天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S85091-5mg

99.06%

￥100.00

S85091-10mg

99.06%

￥130.00

S85091-25mg

99.06%

￥200.00

S85091-100mg

≥99%

￥360.00

货期：2-3天

产品描述：

NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK[1]. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage

靶点：

IC50: 12 nM (CerK); apoptosis;Apoptosis;ERK

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 IC50 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 IC50 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

参考文献：

1. Graf C, et al. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol Pharmacol. 2008 Oct;74(4):925-32. 2. Graf C, et al. A secondary assay for ceramide kinase inhibitors based on cell growth inhibition by short-chain ceramides. Anal Biochem. 2009 Jan 1;384(1):166-9. 3. Pastukhov O,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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.317 ml	11.586 ml	23.172 ml
5 mM	0.463 ml	2.317 ml	4.634 ml
10 mM	0.232 ml	1.159 ml	2.317 ml
50 mM	0.046 ml	0.232 ml	0.463 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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