MIRA-1

MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

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

IC50: 10 μM (Saos-2 His273)[1]

MIRA-1 suppresses growth of Saos-2-His273 cells expressing mutant p53[1]. MIRA-1 (25 μM; 48 hours) inhibits cell growth in a mutant p53-dependent manner[1]. MIRA-1 (5 μM; 14 days) dramatically reduces the number of colonies formed by His273-expressing Saos-2 cells, but is much less efficient in inhibiting p53-null Saos-2 cells[1]. MIRA-1 (10 μM; 48 hours) causes a substantial increase in the fraction of Saos-2 and Saos-2-His273 cells with a sub-G1 DNA content in the presence of mutant p53[1]. MIRA-1 (5 and 10 μM; 24 hours) induces EGFP expression, MDM2 and Bax in SKOV-His175 cells[1]. Cell Proliferation Assay Cell Line: Saos-2-His273, H1299-His175, SKOV-His175 and SKOV-His273[1] Concentration: 25 μM Incubation Time: 48 hours Result: Inhibited cell growth in a mutant p53-dependent manner, with survival rate of 18.5~39% in no doxycycline and 71.5~87.5% in doxycycline. Apoptosis Analysis Cell Line: Saos-2 and Saos-2-His273 cells[1] Concentration: 10 μM Incubation Time: 48 hours Result: Caused a substantial increase in the fraction of cells with a sub-G1 DNA content in the presence of mutant p53.

[1]. Bykov VJ, et al. Reactivation of mutant p53 and induction of apoptosis in human tumor cells by maleimide analogs [published correction appears in J Biol Chem. 2017 Dec 1;292(48):19607]. J Biol Chem. 2005;280(34):30384-30391.