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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-Inauhzin
Inauhzin

Chemical Structure : Inauhzin

CAS No.: 309271-94-1

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Inauhzin (INZ)

货号: PC-38473Not For Human Use, Lab Use Only.

Inauhzin (INZ) is a small molecule SIRT1 inhibitor that effectively reactivates p53, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Inauhzin (INZ) is a small molecule SIRT1 inhibitor that effectively reactivates p53, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress.
Inauhzin (INZ) induced p53 levels as effectively as actinomycin D (ActD, 10 nM), did not apparently affect the interaction between either MDMX and p53, or MDM2 and MDMX, or MDM2 and p53.
Inauhzin inhibited cell growth in a p53-dependent fashion against human lung cancer H460, A549, H1299, colon cancer HCT116, HT29 (IC50=5-50 uM), induceed p53 level and activity as well as p53-dependent apoptosis.
Inauhzin (INZ) stabilizes p53 without either directly inhibiting MDM2-mediated ubiquitylation or causing genotoxicity.
Inauhzin (INZ) effectively inhibits SIRT1 deacetylase activity at 3 uM, directly binds to SIRT1 in vitro, induces p53 acetylation at lysine 382 at 2 uM in cells.
Inauhzin (INZ) induces p53 and p53-dependent apoptosis in vivo and suppresses the growth of human xenograft tumours.

物理化学性质&存储条件

分子量 469.581
分子式 C25H19N5OS2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one

参考文献

1. Zhang Q, et al. EMBO Mol Med. 2012 Apr;4(4):298-312.

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