| Bioactivity | 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[2]. | ||||||||||||
| Invitro | 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[3].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[3].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[3].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[3]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| Name | NVP 231 | ||||||||||||
| CAS | 362003-83-6 | ||||||||||||
| Formula | C25H25N3O2S | ||||||||||||
| Molar Mass | 431.55 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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