1. Apoptosis
    Autophagy
  2. MDM-2/p53
    Autophagy
  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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
25 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 468 In-stock
Estimated Time of Arrival: December 31
100 mg USD 828 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of PRIMA-1Met:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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

APR-246 inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by APR-246 irrespective of p53 status. APR-246 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 APR-246 (PRIMA-1MET), MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog APR-246 promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. APR-246 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
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
Kinase Assay
[1]

Cells are plated in six-well plates at a density of 15 000 cells per cm2. Next day, cells are treated with different concentrations of APR-246 (0, 25, 50, 75 and 100 μM) and harvested after 4, 12 and 24 h. The cells are lysed, and the clarified supernatants are used for either analysis of TrxR enzymatic activities or western blot. Total protein concentrations are determined with a Bradford reagent kit. Cellular TrxR activity is measured using an adapted Trx-dependent end point insulin reduction assay for microwell plates[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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

Purity: >99.0%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PRIMA-1Met
Cat. No.:
HY-19980
Quantity:

PRIMA-1Met

Cat. No.: HY-19980