| 中文名称: | Cambinol | 中文别名: | Cambinol |
|---|---|---|---|
| 英文名称: | Cambinol | CAS: | 14513-15-6 |
| 产品分类: | 小分子化合物 | 纯度: | ≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IC2130 | 索莱宝 | ≥98% | 5mg | 有现货 | 980.00 元 |
| IC2130 | 索莱宝 | ≥98% | 10mg | 有现货 | 1,740.00 元 |
| IC2130 | 索莱宝 | ≥98% | 25mg | 有现货 | 3,603.00 元 |
| IC2130 | 索莱宝 | ≥98% | 50mg | 有现货 | 4,919.00 元 |
| 标准名称: | 英文名称: | Cambinol | |
|---|---|---|---|
| CAS: | 14513-15-6 | 分子式: | C21H16N2O2S |
| 分子量: | 360.428943634033 | 颜色与性状: | |
| 密度: | 1.41 | 沸点: | 667°Cat760mmHg |
| 熔点: | 水溶性: |
| CAS | 14513-15-6 |
| 英文名称 | Cambinol |
| 别名 | ;Cambinol;驱虫速; |
| 分子式 | C21H16N2O2S |
| 分子量 | 360.43 |
| 规格 | 10mg ; 5mg ; 25mg ; 50mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| 运输条件 | 冷藏运输 |
| MDL | MFCD09057543 |
| SMILES | O=C(C(CC1=C2C=CC=CC2=CC=C1O)=C(C3=CC=CC=C3)N4)NC4=S |
| 靶点 | Sirtuin |
| 通路 | Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
| 背景说明 | Cambinol是一种新型的、非竞争性的nSMase2抑制剂。 |
| 生物活性 | Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1-2]. |
| In Vitro | Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis,which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5(42% inhibition at 300 μM)and no activity against SIRT3[1]. |
| In Vivo | Cambinol is well tolerated in mice(100 mg/kg)and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents[1]. |
| 细胞实验 | .The reporter construct with or without varying amounts of GAL4-BCL6 expression plasmid are introduced into NCI-H460 cells using calcium phosphate method. A plasmid containing cytomegalovirus(CMV)-driven β-galactosidase reporter(50 ng)is cotransfected to control for transfection efficiency. Sixteen hours after transfection,cells are treated with 100 μM cambinol of DMSO(control)for 24 hours and the luciferase and β-galactosidase activity is measured[1]. |
| 动物实验 | Mice: Cambinolat the dose of 100 mg/kg,or vehicle are administered i.v. through tail vein injection or i.p. daily from day 5 to 19(five injections per week). The dose of 100 mg/kg cambinol is the highest dose that could be administered as a single i.v. injection due to limited solubility of the drug. Tumor size is measured thrice a week using caliper and the tumor volumes are calculated[1]. |
| 数据来源文献 | [1]. Heltweg B, et al. Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. Cancer Res. 2006 Apr 15;66(8):4368-77. [2]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330. |
| 单位 | 瓶 |
| 1mM-5mg | 13.8723mL |
| 1mM-1mg | 2.7745mL |
| 1mM-10mg | 27.7446mL |
| 5mM-1mg | 0.5549mL |
| 5mM-5mg | 2.7745mL |
| 5mM-10mg | 5.5489mL |
| 10mM-1mg | 0.2774mL |
| 10mM-5mg | 1.3872mL |
| 10mM-10mg | 2.7745mL |
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| 企业认证: | 已认证 | 企业性质: | 生产研发 |
|---|---|---|---|
| 主营产品: | Cibinetide ; NFAT Inhibitor-1 ; N-Myristoyl-Lys-Arg-Thr-Leu-Arg ; Nocistatin(Bovine) ; OXA(17-33) ; | 供货范围: | 试剂 |
| 产品目录: | 119906 | 品牌: | 索莱宝 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| ≥95% | 索莱宝 | 10mg / 5mg / 1mg | 北京 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| ≥95% | 索莱宝 | 10mg / 1mg / 5mg | 北京 |