gn25

GN25 is a specific p53-Snail binding inhibitor with antitumor effects[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> MDM-2/p53

GN25 (10 and 20 μM; 24 h) inhibits cell viability of K-Ras-mutated MEF cells[1]. GN25 (5 μM; 4 h) activates p53 in a K-Ras-dependent manner[1]. GN25 (1-10 μM; 1-6 h) induces p53 and p21 in a dose- and time- dependent manner in K-Ras-mutated A549 and HCT116 cell lines[1]. GN25 activates wild-type p53 in p53WT/MT cells[1]. GN25 (0.25 μM) recovers the masking effect of p53 on CK1/GSK3b-mediated Snail phosphorylation[1]. Cell Viability Assay[1] Cell Line: HCT116, A459 and MKN45 cell lines Concentration: 10 μM Incubation Time: 24 h Result: Obviously suppressed the cell viability of HCT116 and A459 cell lines. Cell Proliferation Assay[1] Cell Line: K-Ras-transformed and N-Ras/Myc-transformed MEF cells Concentration: 10 μM and 20 μM Incubation Time: 24 h Result: Inhibited the viability of K-Ras-transformed but not N-Ras/Myc-transformed MEF cells. Western Blot Analysis[1] Cell Line: K-Ras-MEF, N-Ras/Myc-MEF and Nontransformed MEF cells Concentration: 5 μM Incubation Time: 4 h Result: Only induced p53 and p21 in K-Ras-MEF cells. Western Blot Analysis[1] Cell Line: K-Ras-mutated A549, HCT116 cell lines and MKN45 Concentration: 1, 5, and 10 μM Incubation Time: 1, 3, and 6 h Result: Induced p53 and p21 in a dose- and time- dependent manner in A549 and HCT116 cells.

GN25 (10 and 20 mg/kg; i.p. once a week for 10 weeks) blocks the tumor progression and induces tumor regression in mice[1]. Animal Model: Athymic mice with A549 xenografts[1] Dosage: 10 and 20 mg/kg Administration: Intraperitoneal injection; once a week for 10 weeks Result: Obviously regressed tumors in mice. Showed no significant toxicity in liver, pancreas and kidney.