MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 suppresses growth of Saos-2-His273 cells expressing mutant p53. MIRA-1 induces p53 transcriptional transactivation of p21, MDM2 and PUMA, and promotes tumor cell death by apoptosis in a mutant p53-dependent manner in vitro (IC50 = 10μM).
| Molecular Weight | 183.16 |
| Formula | C8H9NO4 |
| CAS Number | 72835-26-8 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related p53 Products |
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SCH529074 is an orally active, potent activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. |
| BAY 1892005
BAY 1892005, a p53 protein modulator, is active on p53 condensates and does not lead to mutant p53 reactivation. |
| FOXO4-DRI
FOXO4-DRI is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. |
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