Tenovin-1 – CAS 380315-80-0 – Calbiochem

Descrição detalhada : A cell-permeable benzoylthiourea compound that acts as a reversible inhibitor of class III HDAC sirtuins (IC50 against SirT2 ~10 µM). Based on studies using the more soluble analog Tenovin-6, Tenovin-1 is expected not to compete with substrate binding and display lower potency against SirT1/3 (IC50 = 21/67 µM using Tenovin-6). Tenovin-1 (10 µM) up-regulates cellular p53 protein, but not mRNA, level in MCF-7 (>=6-fold in 6 h), presumably by blocking mdm2-mediated p53 degradation. Two day Tenovin-1 treatment (10 µM) results in selective killing of cancer cells with functional p53, but not p53-lacking cancer cells or normal human dermal fibroblasts. Despite its low aqueous solubility, administration of Tenovin-1 suspension is shown to effectively reduce BL2 and ARN8 xenographs in mice in vivo (>=50% reduction with 92 mg/kg daily i.p.)., A cell-permeable benzoylthiourea compound that acts as a reversible inhibitor of class III HDAC sirtuins against SirT2 (IC50 = ~ 10 µM). Based on studies using the more soluble analog Tenovin-6, Tenovin-1 is expected not to compete with substrate binding and display lower potency against SirT1/3 (IC50 = 21/67 µM using Tenovin-6). Tenovin-1 (10 µM) up-regulates cellular p53 protein, but not mRNA, level in MCF-7 (>=6-fold in 6 h), presumably by blocking mdm2-mediated p53 degradation. Two day Tenovin-1 treatment (10 µM) results in selective killing of cancer cells with functional p53, but not p53-lacking cancer cells or normal human dermal fibroblasts. Despite its low aqueous solubility, administration of Tenovin-1 suspension is shown to effectively reduce BL2 and ARN8 xenographs in mice in vivo (>=50% reduction with 92 mg/kg, daily, i.p.).
Sinónimos : Tenovin-1 - CAS 380315-80-0 - Calbiochem; N-(4- tert-Butylbenzoyl)-N?-(4-acetylaminophenyl)-thiourea, SIRT2 Inhibitor V; N-(4-tert-Butylbenzoyl)-N?-(4-acetylaminophenyl)-thiourea, SIRT2 Inhibitor V
Fórmula molecula r: C20H23N3O2S
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG