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NVP 231

CAS No. : 362003-83-6

MCE 国际站：NVP 231

产品活性：NVP 231 是一种强效、特异、可逆的神经酰胺激酶 (CerK) 抑制剂 (IC₅₀=12 nM)，可竞争性地抑制神经酰胺与 CerK 的结合。NVP 231 通过增加 DNA 片段和 caspase-3 和 caspase-9 的裂解来诱导细胞凋亡 (apoptosis)。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: 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.

相关产品：Apoptosis Compound Library | Anti-Cancer Compound Library | Bioactive Compound Library Plus | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Sorafenib | SP600125 | Staurosporine | Angiotensin II human | 5-Fluorouracil | Trametinib | Acetylcysteine | MK-2206 dihydrochloride | Bortezomib | Tamoxifen | Gemcitabine | Pexidartinib | 2-Deoxy-D-glucose | Temozolomide | Ruxolitinib | Verteporfin | Decitabine | BAY 11-7082 | Mdivi-1 | Etoposide | DAPT | Dasatinib | Docetaxel

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