2. Apoptosis Autophagy
  3. MDM-2/p53 Autophagy Apoptosis Ferroptosis
  4. Eprenetapopt

Eprenetapopt  (Synonyms: APR-246; PRIMA-1Met)

製品番号: HY-19980 純度: 99.52%
COA 取扱説明書 Technical Support

Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

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CAS 番号 : 5291-32-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 在庫あり
Solution
10 mM * 1 mL in DMSO USD 92 在庫あり
Solid
5 mg $84 在庫あり
10 mg $132 在庫あり
25 mg $264 在庫あり
50 mg $468 在庫あり
100 mg $828 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of Eprenetapopt:

Eprenetapopt 関連抗体

Top Publications Citing Use of Products

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Jul 8.  [Abstract]

    A PCR assay was used to assess the influence of Eprenetapopt (APR-246; 20 µmol/L, 24 hours) on UBE2T mRNA levels in SG2 and GBM22 cells.

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Jul 8.  [Abstract]

    Western blot analysis was conducted to examine the impact of Eprenetapopt (APR-246; 20 µmol/L, 24 hours) on UBE2T protein levels.

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Jul 8.  [Abstract]

    In vivo bioluminescence experiments were conducted using orthotopic xenograft models of human glioma cells (SG2) in nude mice. On the first, third, fifth, and seventh days following the initial imaging session, Eprenetapopt (APR-246) was administered via i.p. injection at a dose of 400 mg/kg. The results indicated that APR-246 treatment inhibited the proliferation of SG2 cells (Left). Survival analysis revealed that the APR-246 treatment prolonged the survival of nude mice (Right).

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Jul 8.  [Abstract]

    IHC staining of intracranial tumors in nude mice demonstrated that Eprenetapopt (APR-246; ip; 400 mg/kg; On the first, third, fifth, and seventh days following the initial imaging session) treatment decreased the protein levels of both UBE2T and Ki-67.

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2025 Jul 8.  [Abstract]

    IF was used to evaluate the effect of Eprenetapopt (APR-246 ) treatment (20 µmol/L, 24 hours) on the distribution and expression of fibrillarin in SG2 and GBM22 cells.

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Sep 16;8(37):eabm9427.  [Abstract]

    Percentage (%) of dead cells [as determined by % PI+ cells] and percentage of cell confluency following treatment for 24 hours with 50 μM Eprenetapopt with or without 50 μM zVAD-FMK (pan-caspase inhibitor), 12.5 μM Fer-1 (lipophilic antioxidant), 6.25 μM CPX (iron chelator), or 2.5 mM NAC (cysteine supplement) in H1299 (left) and FLO-1 cells (right).

    Eprenetapopt purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Sep 16;8(37):eabm9427.  [Abstract]

    Eprenetapopt (50 μM 24 h) induced ferroptosis in H1299 and FLO-1 cells.

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    製品説明

    Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance[1][2][3].

    IC50 & Target

    p53 activator[1]
    TrxR1 inhibitor[1]
    体外実験

    Eprenetapopt inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by Eprenetapopt irrespective of p53 status. Eprenetapopt 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 Eprenetapopt, MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog Eprenetapopt promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. Eprenetapopt has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53[1].
    Eprenetapopt is a powerful apoptosis-inducing agent. Eprenetapopt can enhance apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. Eprenetapopt treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that Eprenetapopt 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 Eprenetapopt without the induction of p53 target genes.Eprenetapopt regularly induces apoptosis in mutant p53 expressing cells[2].

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

    Eprenetapopt 関連抗体
    分子量

    199.25

    分子式

    C10H17NO3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C(COC)(CO)N2CCC1CC2
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

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

    DMSO : 50 mg/mL (250.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (12.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (12.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (501.88 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.52%

    COA (254 KB) HNMR (258 KB) RP-HPLC (246 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 5.0188 mL 25.0941 mL 50.1882 mL 125.4705 mL
    5 mM 1.0038 mL 5.0188 mL 10.0376 mL 25.0941 mL
    10 mM 0.5019 mL 2.5094 mL 5.0188 mL 12.5471 mL
    15 mM 0.3346 mL 1.6729 mL 3.3459 mL 8.3647 mL
    20 mM 0.2509 mL 1.2547 mL 2.5094 mL 6.2735 mL
    25 mM 0.2008 mL 1.0038 mL 2.0075 mL 5.0188 mL
    30 mM 0.1673 mL 0.8365 mL 1.6729 mL 4.1824 mL
    40 mM 0.1255 mL 0.6274 mL 1.2547 mL 3.1368 mL
    50 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5094 mL
    60 mM 0.0836 mL 0.4182 mL 0.8365 mL 2.0912 mL
    80 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5684 mL
    100 mM 0.0502 mL 0.2509 mL 0.5019 mL 1.2547 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Eprenetapopt Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Eprenetapopt5291-32-7APR-246 PRIMA-1MetAPR246APR 246MDM-2/p53AutophagyApoptosisFerroptosisInhibitorinhibitorinhibit

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