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。
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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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| Cas No. | 362003-83-6 | SDF | |
| Chemical Name | N-(2-benzamido-1,3-benzothiazol-6-yl)adamantane-1-carboxamide | ||
| Canonical SMILES | C1C2CC3CC1CC(C2)(C3)C(=O)NC4=CC5=C(C=C4)N=C(S5)NC(=O)C6=CC=CC=C6 | ||
| Formula | C25H25N3O2S | M.Wt | 431.55 |
| 溶解度 | ≥ 87.6 mg/mL in DMSO with ultrasonic, ≥ 2.58 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3172 mL | 11.5861 mL | 23.1723 mL |
| 5 mM | 0.4634 mL | 2.3172 mL | 4.6345 mL |
| 10 mM | 0.2317 mL | 1.1586 mL | 2.3172 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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