纯度:98% by TLC;NMR (Conforms)
分子式:C14H12O3S2
分子量:292.37
溶剂:DMSO (20 mg/ml)
性状:Yellow solid
存储:-20°C
Activity (short version):p53 activator
Function / Pharmacology:RITA (reactivation of p53 and induction of tumor cell apoptosis) binds to p53 (Kd = 1.5 nM), changing its conformation, preventing it from binding to HDM2 (human ortholog of MDM2, Mouse Double-Minute clone 2), and targeting it for proteasomal degradation.1 It also weakly (computed Kd = 22 μM) binds HDM2 in the cleft that contacts the p53 transactivation domain.2 Its restoration of mutant p53 function depends on eIF2α phosphorylation, and it induces apoptosis via p53-dependent and -independent (JNK/SAPK/p38; protein translation) pathways.3-5 Induces senescence in head and neck cancer cells.6