1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. 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.

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

HET0016 Chemical Structure

HET0016 Chemical Structure

CAS No. : 339068-25-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 95 In-stock
25 mg USD 190 In-stock
50 mg USD 350 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

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.
Molecular Weight

206.28

Formula

C12H18N2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

  • Molarity Calculator

  • Dilution Calculator

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 in Saline

    Solubility: 2 mg/mL (9.70 mM); Clear solution; Need ultrasonic

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
Purity & Documentation
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, 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.

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Product Name:
HET0016
Cat. No.:
HY-124527
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