NVP 231 |
| カタログ番号GC13566 |
NVP 231 は、セラミドの CerK への結合を競合的に阻害する、強力で特異的かつ可逆的なセラミドキナーゼ (CerK) 阻害剤 (IC50 = 12 nM) です。 NVP 231 は、DNA の断片化とカスパーゼ 3 およびカスパーゼ 9 の切断を増加させることにより、細胞のアポトーシスを誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 362003-83-6
Sample solution is provided at 25 µL, 10mM.
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NVP 231 is a potent, reversible and specific inhibitor of ceramide kinase(CerK) with the IC50 value of 12±2nM in radio assay [1].
NVP 231 has been noted to inhibit CerK with the IC50 value of 12±2nM and have the 90% inhibition at 100 nM in the radio assay. In addition, NVP 231 has been reported to compete with ceramide with the Ki value of 7.4 nM. Furthermore, NVP 231 has been revealed to achieve complete inhibition of CIP at 100nM. NVP 231 in an assay based on human CerK-overexpressing COS-cells (COS-CerK). And the study has been exhibited that NVP 231 is a more potent inhibitor of mouse CerK. Apart from these, NVP 231 has been shown the specificity to CerK with the IC50 values of 0.01 μM, 100 μM, >100 μM, 5 μM, >25 μM, >25 μM, >10 μM, >10 μM and >10 μM for hCerK, hSphK1, hSphK2, hDAGKα, hPI3Kα, hVps34, hGCS, hSMS-1 and CERT, respectively [1].
References:
[1]Graf C1, 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.
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