YF-2 是一种高选择性,可透过血脑屏障的组蛋白乙酰转移酶激动剂,能够在海马区乙酰化 H3,对 CBP、PCAF 和 GCN5 的EC50值分别为 2.75、29.04 和 49.31 μM,具有抗肿瘤和抗阿尔滋海默症的活性。
产品描述
YF-2 is blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, CBP, PCAF, and GCN5 with EC50s of 2.75 μM, 29.04 μM and 49.31 μM , respectively
体外活性
YF-2 (0.03, 0.1, 0.25, 0.5, 1, 2.5, 5, 15, 40 and 80 μM, 72 hours) inhibits the preliferation of U251, CCRF-CEM, Hs578T, NCI-ADR-RES cells, respectively.
体内活性
YF-2 (20 mg/kg, 2 hours befor electric shock or 5 mg/kg, 30 min before the electric shock, i.p.) rescues the defect in contextual memory in mice, and exhibits no effect on contextual memory alone at 20 mg/kg in mice.
Cas No.
1311423-89-8
分子式
C20H22ClF3N2O3
分子量
430.85
储存和溶解度
DMSO:125 mg/mL (290.12 mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years