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Submit ReviewCambinol is a neutral sphingomyelinase-2 (nSMase2) inhibitor (Ki = 7 μM; IC50 ~ 7.7 μM). In vitro, Cambinol suppresses extracellular vesicle production and inhibits cell-to-cell tau propagation in tau biosensor cells. In vivo, Cambinol decreases tumor necrosis factor-α or interleukin-1β-induced increases of ceramide and cell death in primary neurons. Cambinol is neuroprotective and brain penetrant. Cambinol inhibits the activity of human SIRT1 and SIRT2 and exerts antitumor activity in vitro and in mouse xenograft studies.
分子量 | 360.43 |
公式 | C21H16N2O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 14513-15-6 |
PubChem ID | 3246390 |
InChI Key | RVNSQVIUFZVNAU-UHFFFAOYSA-N |
Smiles | OC1=C(C2=CC=CC=C2C=C1)CC3=C(C4=CC=CC=C4)NC(NC3=O)=S |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.04 | 100 |
以下数据基于产品分子量 360.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.77 mL | 13.87 mL | 27.74 mL |
5 mM | 0.55 mL | 2.77 mL | 5.55 mL |
10 mM | 0.28 mL | 1.39 mL | 2.77 mL |
50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Figuera-Losada et al (2015) Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties. PLoS One 10 e0124481 PMID: 26010541
Stepanek et al (2019) Neutral sphingomyelinase 2 inhibitors based on the 4-(1H-imidazol-2-yl)-2,6-dialkoxyphenol scaffold. Eur.J.Med.Chem. 170 276 PMID: 30921693
Sackmann et al (2019) Inhibition of nSMase2 reduces the transfer of oligomeric α-synuclein irrespective of hypoxia. Front.Mol.Neurosci. 12 200 PMID: 31555088
Bilousova (2018) Suppression of tau propagation using an inhibitor that targets the DK-switch of nSMase2. Biochem.Biophys.Res.Commun. 499 751 PMID: 29604274
Heltweg et al (2006) Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. Cancer Res. 66 4368 PMID: 16618762
If you know of a relevant reference for Cambinol, please let us know.
关键词: Cambinol, Cambinol supplier, neutral, sphingomyelinase, 2, nSMase2, inhibition, inhibitors, inhibits, Sphingomyelin, SMase, brain, penetrant, SIRT1, SIRT2, antitumor, tau, Other, Hydrolases, Class, III, HDACs, (Sirtuins), 7137, Tocris Bioscience
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