1. Apoptosis
    Autophagy
  2. MDM-2/p53
    Autophagy
    Apoptosis
    Ferroptosis
  3. PRIMA-1Met

PRIMA-1Met (Synonyms: APR-246)

Cat. No.: HY-19980 Purity: >99.0%
Handling Instructions

PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

For research use only. We do not sell to patients.

PRIMA-1Met Chemical Structure

PRIMA-1Met Chemical Structure

CAS No. : 5291-32-7

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

IC50 & Target

p53 activator[1]
TrxR1 inhibitor[1]

In Vitro

PRIMA-1Met inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by PRIMA-1Met irrespective of p53 status. PRIMA-1Met can directly affect cellular redox status via targeting of TrxR1. Several small molecules have been shown to restore wild-type activity to mutant p53, including CP-31398, PRIMA-1 and PRIMA-1MET, MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog PRIMA-1Met promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. PRIMA-1Met has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53[1]. PRIMA-1MET is a powerful apoptosis-inducing agent. PRIMA-1MET can enhance apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. PRIMA-1MET treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that PRIMA-1MET can also act independently of the p53 status of the cell. It can radiosensitize prostate carcinoma cell lines with mutant or wild type p53 and p53-/- cells as well. Introduction of mutant p53 (p53ser249 or p53gln248) into p53-/- hepatocarcinoma cells increases sensitivity to PRIMA-1MET without the induction of p53 target genes. PRIMA-1MET regularly induces apoptosis in mutant p53 expressing cells[2].

Clinical Trial
Molecular Weight

199.25

Formula

C₁₀H₁₇NO₃

CAS No.

5291-32-7

SMILES

O=C1C(COC)(CO)N2CCC1CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (250.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.0188 mL 25.0941 mL 50.1882 mL
5 mM 1.0038 mL 5.0188 mL 10.0376 mL
10 mM 0.5019 mL 2.5094 mL 5.0188 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: >99.0%

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Keywords:

PRIMA-1MetAPR-246APR246APR 246MDM-2/p53AutophagyApoptosisFerroptosisInhibitorinhibitorinhibit

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PRIMA-1Met
Cat. No.:
HY-19980
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