Salermide

Research use only, not for human use.

A potent Sirtuin inhibitor with IC50 of 76 and 45 uM for SIRT1 and SIRT2, respectively.

A potent Sirtuin inhibitor with IC50 of 76 and 45 uM for SIRT1 and SIRT2, respectively; prompts tumour-specific cell death in a wide range of human cancer cell lines (MCF cells at 50 uM), causes cell cycle arrest at G(1), results in the in vivo acetylation of the SIRT1/2 target p53, but not EX527.

Salermide shows a dose-dependent inhibition that rises to 80% at 90 μM and 25 μMagainst Sirt1 and Sirt2, respectively. Salermide can prompt tumour-specific cell death in a wide range of human cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231). Incubation with 100 μM Salermide alone resulted in an increase of cytosolicactivated caspase 3 and a decrease of mitochondrialcytochrome. Salermide alone can induce apoptosis through both extrinsic and intrinsic pathways. Salermide had several antitumorigenic advantages over the earlier described class III HDAC inhibitors: firstly, it mimics the universal proapoptotic effect on cancer samples exhibited by the classical class I, II and IV HDAC inhibitors, and secondly, its proapoptotic effect is cancer-specific.

Salermide is well tolerated by mice at concentrations up to 100 μM. Salermide's mechanism of action in vivo is specifically mediated by Sirt1. Intraperitoneal feeding of Salermide has no apparent toxicity in nude mice.

Salermide

Chromatin/Epigenetic

Sirtuin

SIRT1|SIRT2

Cancer

——

1105698-15-4

394.46508

C26H22N2O2

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC=CC(/N=C/C2=C3C=CC=CC3=CC=C2O)=C1)C(C)C4=CC=CC=C4

Benzeneacetamide, N-[3-[[(2-hydroxy-1-naphthalenyl)methylene]amino]phenyl]-α-methyl-

(-20℃)

With Ice Pack

≥ 2 years