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Inauhzin

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Catalog No.
B3272
SIRT1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
10mg
¥ 990.00
现货
50mg
¥ 2,990.00
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Background

Inauhzin is a small-molecule inhibitor of SIRT1 with IC50 value of 0.7-2μM [1].

Inauhzin inhibits SIRT1 deacetylation activity and subsequently activates the substrate of SIRT1, p53, in a dose-dependent manner. It shows an induction of acetylation of p53 and Histone H3 in the K382 and K9 residues, respectively. The inhibition of SIRT1 is selective. It has no significant effect on SIRT2, SIRT3 or HDAC8 in the Fluor-de-Lys fluorimetric assay. Since it is an activator of p53, inauhzin inhibits cell growth in different p53-containing human cancer cells including H460, H1299, A549, HT29 and WI38. The IC50 values are 5.4μM, 51.9μM, 3.2μM, 33.9μM and 85.4μM, respectively. Furthermore, inauhzin induces cell apoptosis through activating p53. In the xenograft tumours derived from H460 cells, inauhzin also significantly induces p53 activity and p53-dependent apoptosis at 2μM [1].

References:
[1] Zhang Q, Zeng SX, Zhang Y, Zhang Y, Ding D, Ye Q, Meroueh SO, Lu H. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol Med. 2012 Apr;4(4):298-312.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt469.58
Cas No.309271-94-1
FormulaC25H19N5OS2
Solubility≥23.5mg/mL in DMSO
Chemical Name2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one
SDFDownload SDF
Canonical SMILESCCC(SC1=NC2=C(N=N1)C3=CC=CC=C3N2)C(N4C5=CC=CC=C5SC6=CC=CC=C64)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

Cell experiment [1]:

细胞系

H460、H1299、A549、HT29和WI38

溶解方法

该化合物在DMSO中的溶解度大于23.5 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

2 μM,18h

应用

Inauhzin以剂量依赖性方式抑制不同的含p53的人类癌细胞(包括H460、H1299、A549、HT29和WI38)的细胞生长。Inauhzin通过抑制SIRT1活性有效地重激活p53,促进人类癌细胞的p53依赖性细胞凋亡,不引起明显的遗传毒性应激。此外,INZ通过增加p53乙酰化和预防细胞中MDM2介导的p53泛素化来稳定p53。INZ抑制细胞增殖,诱导衰老和肿瘤特异性凋亡。

动物实验 [1]:

动物模型

携带H460或HCT116异种移植物的雌性SCID小鼠

给药剂量

腹腔注射,18h,2 μM

应用

在携带p53的H460和HCT116细胞的异种移植肿瘤的小鼠中,Inauhzin抑制肿瘤生长,而对正常组织和SCID肿瘤小鼠没有明显的毒性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Zhang Q, Zeng S X, Zhang Y, et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53[J]. EMBO molecular medicine, 2012, 4(4): 298-312.

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