MIRA-1 - ≥99%, high purity , CAS No.72835-26-8

Item Number

M275724

• Synonyms: NSC 19630 | MIRA-1 | (2,5-dihydro-1H-pyrrol-1-yl)methyl propionate | BS-45665 | CCG-37541 | NCI19630 | WRN Helicase Inhibitor, NSC 19630 - CAS 72835-26-8 | 1-[(1-Oxopropoxy)methyl]-1H-pyrrole 2,5-dione | N-(Propionyloxymethyl)maleimide; NSC 19630 | (2,5-d
• Specifications & Purity: ≥99%
• Biochemical and Physiological Mechanisms: Novel, nontoxic and selective p53 inducer. Antitumor agent. Promotes tumor cell apoptosis in a mutant p53-dependent manner (IC 50 = 10 μM) and prolongs survival. Active in vivo and in vitro .
• Storage Temp: Store at 2-8°C
• Shipped In: Wet ice
• Note: Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Product Description

A cell-permeable maleimide compound selectively inhibits Werner syndrome WRN helicase activity (IC50 = 20 µM) over its ATPase and exonuclease activities (19% and <10% inhibition, respectively, at 50 µM), while exhibiting no effect against the helicase activity of two other human RecQ family DNA helicases (RECQ1 and Werner syndrome BLM), Fanconi anemia group J helicase FANCJ, as well as three other E. coli helicases, RecQ, UvrD, and DnaB. The WRN-dependent antiproliferation activity of MIRA-1/NSC 19630 in HeLa 1.2.11 cultures (0% vs. 95% inhibition with or without siRNA-mediated WRN-depletion, respectively, after 48 h 3 µM treatment) is shown to be a direct result of apoptosis induction due to replication forks blockage (20-fold increase in PCNA foci staining after 72 h 2 µM treatment), enhanced DSB (17-fold increase in γ-H2AX foci staining after 72 h 2 µM treatment), and increased S-phase population (from 24% to 42% after 72 h 2 µM treatment). In some cells, MIRA-1/NSC 19630 appears to also exert its apoptotic effect, at least in part, by restoring DNA-binding and transactivation function of some, but not all, p53 mutants.