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

HET0016 

Cat. No.: HY-124527 Purity: 99.78%
Handling Instructions

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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10 mM * 1  mL in DMSO USD 61 In-stock
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25 mg USD 190 In-stock
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50 mg USD 350 In-stock
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100 mg USD 650 In-stock
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Based on 1 publication(s) in Google Scholar

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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

17.7 nM (CYP4A1), 12.1 nM (CYP4A2), 20.6 nM (CYP4A3)[1], CYP450[2]

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].

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].

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.

339068-25-6

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

DMSO : 5 mg/mL (24.24 mM; Need ultrasonic)

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
10 mM 0.4848 mL 2.4239 mL 4.8478 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

HET0016HET 0016HET-0016Cytochrome P450CYPs20-HETE20-hydroxyeicosatetraenoicacid,CYP450CYP4A1CYP4A2CYP4A3Inhibitorinhibitorinhibit

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HET0016
Cat. No.:
HY-124527
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