Chemical Name: 5,5-(2,5-Furandiyl)bis-2-thiophenemethanol. Alternate Names: NSC 652287
p53 activator
Molecular Weight:
292.37
Purity:
98% by TLC NMr (Conforms)
Form:
Yellow solid
CAS Number:
[213261-59-7]
Formula:
C14H12O3S2
Application Notes:
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 eIF2alpha 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
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