PRIMA-1Met
SIGMA/SML1789 - ≥98% (HPLC)
Synonym: 2-
CAS Number: 5291-32-7
Empirical Formula (Hill Notation): C10H17NO3
Molecular Weight: 199.25
Linear Formula: C10H17NO3
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to beige |
form | powder |
Quality Level | 100 ![]() |
solubility | DMSO: 2 mg/mL, clear |
storage temp. | 2-8°C |
Biochem/physiol Actions: | PRIMA-1Met (APR-246) is a re-activator of mutant p53 activity. It′s the methylated, more potent derivative of PRIMA-1. PRIMA-1Met covalently modifies the core domain of mutated p53 restoring the wild-type conformation and activty of p53 in tumor cells, leading to cell cycle arrest and apoptosis. PRIMA-1Met has also been shown to increase intracellular levels of reactive oxygen species (ROS), which may contribute to its anti-tumor activity. |
Biochem/physiol Actions: | PRIMA-1Met, also called APR-246, is converted to methylene quinuclidinone (MQ), a Michael acceptor. It interacts with p53 through the cysteine (Cys) residue. It blocks the thioredoxin reductase (TrxR1) enzyme. It is under clinical investigation and well-studied. PRIMA-1Met effect is tested on breast cancer specific gene expression. |
Symbol | ![]() |
Signal word | Warning |
Hazard statements | H315 - H319 |
Precautionary statements | P305 + P351 + P338 |
RIDADR | NONH for all modes of transport |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | 2-8°C |
UNSPSC | 12352200 |