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HET0016

Catalog No. T11556   CAS 339068-25-6

HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis). HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.

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HET0016 Chemical Structure
HET0016, CAS 339068-25-6
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Purity: 98.84%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis). HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.
Targets&IC50 CYP4A1:17.7 nM , CYP4A2: 12.1 nM , CYP4A3: 20.6 nM
In vitro HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells .HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A .
In vivo HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment. HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins.HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model. HET0016 reduces the metalloproteinases' levels in the lungs via PI3K/AKT pathway in mice.
Molecular Weight 206.28
Formula C12H18N2O
CAS No. 339068-25-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DCM: 12.5 mg/mL (60.60 mM), sonification is recommended.

DMSO: 5 mg/mL (24.24 mM), sonification is recommended.

TargetMolReferences and Literature

1. Seki T, et al. Cytochrome P450 4A isoform inhibitory profile of N-hydroxy-N'-(4-butyl-2-methylphenyl)-formamidine (HET0016), a selective inhibitor of 20-HETE synthesis. Biol Pharm Bull. 2005 Sep;28(9):1651-4. 2. Borin TF, et al. HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model. PLoS One. 2017 Jun 13;12(6):e0178830. 3. Liu Y, et al. The protective effect of HET0016 on brain edema and blood-brain barrier dysfunction after cerebral ischemia/reperfusion. Brain Res. 2014 Jan 28;1544:45-53.

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Keywords

HET0016 339068-25-6 Others HET 0016 HET-0016 inhibitor inhibit

 

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