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.

HPPE Chemical Structure

HPPE Chemical Structure

CAS No. : 1325721-55-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • 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 : 125 mg/mL (260.70 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

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

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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HPPE
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