2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. HET0016

HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.

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No. CAS : 339068-25-6

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10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 6 publication(s) in Google Scholar

Other Forms of HET0016:

HET0016 Related Antibodies

Top Publications Citing Use of Products

    HET0016 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jul 28;13(7):653.  [Abstract]

    Survival analysis of the indicated mice in CLP-induced sepsis with or without treatment of 10 mg/kg HET0016, 20 mg/kg JSH-23, or 10 mg/kg Carnosol at 2 h before CLP and 12, 24, 48, and 72 h after CLP.

    HET0016 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jul 28;13(7):653.  [Abstract]

    Immunoblot analysis of p-TBK1, TBK1, p-P65, and P65 in PBMCs from patients with sepsis or healthy control, supplemented with or without HET0016 (5 μM) for 24 h.

    HET0016 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Jul 28;13(7):653.  [Abstract]

    qPCR analysis of Il-6, Il-1b, and Tnf mRNA in PBMCs from patients with sepsis or healthy control, supplemented with or without HET0016 (5 μM) for 24 h.

    Ver todos los productos específicos de isoformas Cytochrome P450:

    Ver todas las isoformas
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth[1][2].

    IC50 & Target

    CYP4

     

    In Vitro

    HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A [1].
    HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells [2].

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

    HET0016 Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: MDA-MB-231 cells
    Concentration: 100 μM
    Incubation Time: 24 hours, 48 hours
    Result: Decreased migration and invasion of breast cancer metastatic cells
    In Vivo

    HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model[2].
    HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice[2].
    HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment[2].
    HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins[3].

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

    Animal Model: 4–5 weeks female Balb/c mice (16-18 g)[2]
    Dosage: 10 mg/kg/day
    Administration: Intravenously; 5 days a week; for 3 weeks; starting from day 15 of tumor implantation
    Result: Reduced tumor volume and lung metastasis.
    Peso molecular

    206.28

    Fòrmula

    C12H18N2O
    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCCC1=CC=C(C(C)=C1)/N=C/NO
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DCM : 12.5 mg/mL (60.60 mM; Need ultrasonic)

    DMSO : 5 mg/mL (24.24 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 4.8478 mL 24.2389 mL 48.4778 mL
    5 mM 0.9696 mL 4.8478 mL 9.6956 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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:  20% HP-β-CD/1% Tween-80 in PBS

      Solubility: 2 mg/mL (9.70 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

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

    Purity: 99.69%

    SDS (393 KB)

    COA (242 KB) LCMS (96 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    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
    DMSO / DCM 1 mM 4.8478 mL 24.2389 mL 48.4778 mL 121.1945 mL
    5 mM 0.9696 mL 4.8478 mL 9.6956 mL 24.2389 mL
    10 mM 0.4848 mL 2.4239 mL 4.8478 mL 12.1194 mL
    15 mM 0.3232 mL 1.6159 mL 3.2319 mL 8.0796 mL
    20 mM 0.2424 mL 1.2119 mL 2.4239 mL 6.0597 mL
    DCM 25 mM 0.1939 mL 0.9696 mL 1.9391 mL 4.8478 mL
    30 mM 0.1616 mL 0.8080 mL 1.6159 mL 4.0398 mL
    40 mM 0.1212 mL 0.6060 mL 1.2119 mL 3.0299 mL
    50 mM 0.0970 mL 0.4848 mL 0.9696 mL 2.4239 mL
    60 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0199 mL
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    HET0016 Related Classifications

    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.

    Keywords:

    HET0016339068-25-6HET 0016HET-0016Cytochrome P450CYPs20-HETE20-hydroxyeicosatetraenoicacid,CYP450CYP4A1CYP4A2CYP4A3Inhibitorinhibitorinhibit

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    Inquiry Information

    Nombre del producto:
    HET0016
    Cat. No.:
    HY-124527
    Cantidad:
    MCE Japan Authorized Agent:

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    SAFETY DATA SHEET (SDS)

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