| 產(chǎn)品描述： | Inauhzin是具有細(xì)胞透性的SIRT1抑制劑，IC50為0.7-2 μM，可通過(guò)抑制SIRT1脫乙酰活性重新激活p53 |
| 靶點(diǎn)： |
SIRT1; p53;Sirtuin |
| 體外研究： |
Inauhzin (INZ) is a potent p53 activator and mediates p53-dependent cytotoxicity. INZ inhibits cell proliferation by triggering both apoptosis and senescence in p53-containning cells, though it predominantly induces p53-dependent apoptosis. INZ is able to prevent p53 from MDM2-mediated ubiquitylation and proteasomal degradation and protects p53 without either directly inhibiting MDM2 activity towards p53 or interfering with MDMX/MDM2–p53 interaction. INZ induces acetylation of p53, but not tubulin, in cells[1]. Inauhzin is a (sub)micromolar SIRT1i selective over SIRT2/3 |
| 體內(nèi)研究： |
Inauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53 |
| 細(xì)胞實(shí)驗(yàn)： |
Cell lines: human lung cancer H460, A549, H1299, colon cancer HCT116, HT29, osteosarcoma U2OS and SJSA, breast cancer MCF7, ovarian cancer A2780, IGROV1 and SKOV3 and glioma U87 and U373 cells, as well as human embryonic fibroblast WI-38 and normal human fibroblast (NHF) cells Concentrations: 0-10 μM Incubation Time: 18 h Method: -- |
| 動(dòng)物實(shí)驗(yàn)： |
Animal Models: SCID mice with H460 xenograft tumours Dosages: 30 mg/kg Administration: IP |
| 參考文獻(xiàn)： |
1. Zhang Q, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol Med. 2012, 4(4):298-312. 2. Carafa V, et al. Sirtuin functions and modulation: from chemistry to the clinic. Clin Epigenetics. 2016, 8:61. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.13 ml |
10.648 ml |
21.296 ml |
| 5 mM |
0.426 ml |
2.13 ml |
4.259 ml |
| 10 mM |
0.213 ml |
1.065 ml |
2.13 ml |
| 50 mM |
0.043 ml |
0.213 ml |
0.426 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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北京