1. Metabolic Enzyme/Protease
  2. Mitochondrial Metabolism
  3. HPPE

HPPE (compound 236) is an orally active, potential Bach1 inhibitor. Bach1 is a transcription factor of the cap'n'collar type alkaline region leucine zipper factor family (CNC-bZip) that regulates mitochondrial metabolism and reduces glucose utilization. HPPE can be used for research in psoriasis, multiple sclerosis, and COPD.

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

CAS No. : 1325721-55-8

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    HPPE purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206.  [Abstract]

    Western blot analysis was used to detect the protein and phosphorylation levels of PRC1 in cells after treatment. H1299 cells were subcutaneously injected into nude mice to construct xenografts, followed by intratumoral injections (10 mg/kg: Bobcat339, HPPE, or PLK1-IN-10) starting from day 7.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    HPPE (compound 236) is an orally active, potential Bach1 inhibitor. Bach1 is a transcription factor of the cap'n'collar type alkaline region leucine zipper factor family (CNC-bZip) that regulates mitochondrial metabolism and reduces glucose utilization. HPPE can be used for research in psoriasis, multiple sclerosis, and COPD[1][2][3][4].

    IC50 & Target

    Bach1[1]

    In Vitro

    HPPE (0-20 μM, 18 h) is competitively inhibited by the overexpressed WT Bach1 in HepG2 cells[3].
    HPPE (3 μM, 1 h)-induced Bach1 derepression requires nuclear export of Bach1 and exhibited Nrf2 stabilization activity in M17-5 neuroblastoma cells[3].
    HPPE (10 μM, 8 h) activates NRF2 driven transcription independently of BACH1 in HEK293T cells[4].
    HPPE (10 μM, 1 h) liberates cellular zinc and increases cellular ROS levels in HEK293T cells[4].

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

    Western Blot Analysis[3]

    Cell Line: M17-5 neuroblastoma cells
    Concentration: 3 μM
    Incubation Time: 1 h
    Result: Significantly up-regulated Hmox1 (a Bach1 target) protein levels and showed accumulation of Nrf2 protein in the cytosol and especially in the nucleus in M17-5 neuroblastoma cells.

    Western Blot Analysis[4]

    Cell Line: HEK293T cells
    Concentration: 10 μM
    Incubation Time: 8 h
    Result: Robustly stabilized NRF2 protein levels within 8 hours of treatment in HEK293T cells.
    In Vivo

    HPPE (5 and 10 mg/kg, oral gavage, twice a day for 6 days) ameliorates MPTP-induced dopaminergic neurodegeneration and associated oxidative stress and neuroinflammation in the acute MPTP mouse model[3].

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

    Animal Model: The acute MPTP mouse model[2]
    Dosage: 5 and 10 mg/kg
    Administration: oral gavage, twice a day for 6 days
    Result: Significantly protected SNpc dopaminergic neurons against MPTP neurotoxicity.
    Molecular Weight

    479.48

    Formula

    C21H20F3N5O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC(N=C(N2C)NC3=NC4=C(S3)C=C(C(F)(F)F)C=C4)=C2C=C1)NCCOCCO

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (208.56 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 2.0856 mL 10.4280 mL 20.8559 mL
    5 mM 0.4171 mL 2.0856 mL 4.1712 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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 (5.21 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 (5.21 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.71%

    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0856 mL 10.4280 mL 20.8559 mL 52.1398 mL
    5 mM 0.4171 mL 2.0856 mL 4.1712 mL 10.4280 mL
    10 mM 0.2086 mL 1.0428 mL 2.0856 mL 5.2140 mL
    15 mM 0.1390 mL 0.6952 mL 1.3904 mL 3.4760 mL
    20 mM 0.1043 mL 0.5214 mL 1.0428 mL 2.6070 mL
    25 mM 0.0834 mL 0.4171 mL 0.8342 mL 2.0856 mL
    30 mM 0.0695 mL 0.3476 mL 0.6952 mL 1.7380 mL
    40 mM 0.0521 mL 0.2607 mL 0.5214 mL 1.3035 mL
    50 mM 0.0417 mL 0.2086 mL 0.4171 mL 1.0428 mL
    60 mM 0.0348 mL 0.1738 mL 0.3476 mL 0.8690 mL
    80 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.6517 mL
    100 mM 0.0209 mL 0.1043 mL 0.2086 mL 0.5214 mL
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    Help & FAQs
    • 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.

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