货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T93825-1ml促销	10mM in DMSO	￥920.00 ￥730.00 T93825-1ml ￥730.00 现货	10 10	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T93825-1ml促销

10mM in DMSO

￥920.00 ￥730.00

产品描述：

SIRT1 选择性抑制剂 | 活化剂 | 调节剂;SIRT1 Selective Inhibitors | Activators | Modulators;;InformationInauhzin is a cell-permeableSIRT1inhibitor with an IC50 of 0.7-2 μM and reactivatesp53by inhibiting SIRT1 deacetylation activity.TargetsSIRT1 ; p53In vitroInauhzin (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. Inauhzin is a (sub)micromolar SIRT1i selective over SIRT2/3.In vivoInauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53.Cell Research(from reference)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 Concentrations：0-10 μM Incubation Time：18 h

体内研究：

Inauhzin (30 mg/kg，腹腔注射) 可有效诱导细胞凋亡并抑制携带 p53 的 H460 异种移植瘤的肿瘤生长。
Inauhzin (30 mg/kg，腹腔注射) 可使 HCT116 肿瘤体积缩小约 70%。Inauhzin (15 mg/kg) 与 150 mg/kg Nutlin-3 联合使用，在 HCT116p53+/+ 异种移植瘤中表现出显著的 p53 诱导、细胞凋亡和肿瘤抑制的协同作用。

参考文献：

1. Zhang Q, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol Med. 2012 Apr;4(4):298-312.
2. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth. Cancer Biol Ther. 2012 Aug;13(10):915-24.
3. Nguyen D, et al. Reviving the guardian of the genome: Small molecule activators of p53. Pharmacol Ther. 2017 Oct;178:92-108.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	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：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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