产品描述

Inauhzin是具有细胞透性的SIRT1抑制剂，IC50为0.7-2 μM，可通过抑制SIRT1脱乙酰活性重新激活p53。

靶点（IC50 & Targe）

SIRT1,p53

体外研究

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[2].

体内研究

Inauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53[1].

细胞实验

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:--

(Only for Reference)

动物实验

Animal Models: SCID mice with H460 xenograft tumours

Formulation: 5% DMSO

Dosages: 30 mg/kg

Administration: IP

(Only for Reference)

参考文献

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

[2] Carafa V, et al. Clin Epigenetics. 2016, 8:61.