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My CartCAS：380315-80-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 380315-80-0 |
| Name | Tenovin-1 |
| Molecular Formula | C20H23N3O2S |
| Molecular Weight | 369.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-256-5 |
| MDL | MFCD02914760 |
| SMILES | O=C(NC(NC1=CC=C(NC(C)=O)C=C1)=S)C2=CC=C(C(C)(C)C)C=C2 |
| InChIKey | WOWJIWFCOPZFGV-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H23N3O2S/c1-13(24)21-16-9-11-17(12-10-16)22-19(26)23-18(25)14-5-7-15(8-6-14)20(2,3)4/h5-12H,1-4H3,(H,21,24)(H2,22,23,25,26) |
| PubChem CID | 1013376 |
| Target Point | Sirtuin;p53 |
| Passage | Apoptosis |
| Background | Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, and activates p53. |
| Biological Activity | Tenovin-1 是 sirtuin 1 和 sirtuin 2 的抑制剂，同时可激活 p53，在癌症研究中可能具有潜在的治疗作用。Tenovin-1保护p53免受mdm2介导的降解，对p53合成几乎没有影响。 [1-5] |
| In Vitro | Tenovin-1(1-10μM)在SK-N-MC细胞中诱导钟形浓度依赖性细胞死亡。 Tenovin-1改变Bcl-2家族成员的基因和蛋白质表达。然而，Tenovin-1在较低浓度下对mRNA和蛋白质表达水平的影响比较高浓度更强。此外，Tenovin-1诱导的细胞毒性作用依赖于p53野生型WE-68细胞中的半胱天冬酶，但不依赖于p53无效SK-N-MC细胞中的半胱天冬酶。 AIF在p53无效SK-N-MC细胞中的tenovin-1诱导的细胞死亡中起主要作用，但在p53野生型WE-68细胞中不起作用。活性氧物质也参与SK-N-MC细胞中的tenovin-1介导的细胞死亡。此外，Tenovin-1在SK-N-MC细胞中引起DNA损伤[1]。 Tenovin-1(5μM)增加胶质母细胞瘤细胞和大鼠原代星形胶质细胞的核大小。 Tenovin-1诱导细胞衰老，似乎与细胞死亡无关[2]。 Tenovin-1靶向p53上游的一个因子，不仅调节p53功能，还调节其他细胞通路。 Tenovin-1(10μM)抑制SirT2脱乙酰酶活性[3]。 Tenovin-1(10μM)减少NSCLC细胞的增殖和锚定独立生长。 Tenovin-1还抑制H358肺癌细胞的细胞生长[4]。 |
| In Vivo | Tenovin-1(92 mg/kg，ip)可减少源自BL2细胞或ARN8细胞的SCID小鼠肿瘤的生长[5]。 |
| Cell Experiment | 将细胞接种在96孔板中。用10μMTenovin-1(tnv-1)处理或用siRNA转染。随后测定细胞活力[4]。 |
| Animal Experiment | 将ARN8黑素瘤或BL2伯基特氏淋巴瘤细胞注射到SCID小鼠的侧腹并使其发育直至肿瘤变得可触知。通过腹膜内注射以92.5mg/kg每天(14天)施用Tenovin-1(在70％环糊精中)，并在18天的时间内测量肿瘤生长。对照动物用70％环糊精处理。在BL2实验中，每次治疗n = 12。在ARN8实验中，对照组n = 14，tenovin-1治疗组n = 16。生长测量值在组间平均并绘图[5]。 |
| Data Literature Source | [1]. Marx C，et al. The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death in a p53 null Ewing's sarcoma cell line. Invest New Drugs. 2017 Nov 18. [2]. Yoon KB，et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016 Jun;16(3):183-8. [3]. Lain S，et al. Discovery，in vivo activity，and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. [4]. Grbesa I，et al. Expression of sirtuin 1 and 2 is associated with poor prognosis in non-small cell lung cancer patients. PLoS One. 2015 Apr 27;10(4):e0124670. [5]. Lain S，et al. Discovery，in vivo activity，and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. |
| Unit | Piece |
| Specification | 5mg 10mg 25mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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