HET-0016

Modify Date: 2024-01-06 13:03:19

HET-0016 Structure
HET-0016 structure
Common Name HET-0016
CAS Number 339068-25-6 Molecular Weight 206.284
Density 1.0±0.1 g/cm3 Boiling Point 356.9±52.0 °C at 760 mmHg
Molecular Formula C12H18N2O Melting Point N/A
MSDS N/A Flash Point 169.7±30.7 °C

 Use of HET-0016


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].

 Names

Name N'-(4-butyl-2-methylphenyl)-N-hydroxymethanimidamide
Synonym More Synonyms

 HET-0016 Biological Activity

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].
Related Catalog
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.
References

[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.

 Chemical & Physical Properties

Density 1.0±0.1 g/cm3
Boiling Point 356.9±52.0 °C at 760 mmHg
Molecular Formula C12H18N2O
Molecular Weight 206.284
Flash Point 169.7±30.7 °C
Exact Mass 206.141907
PSA 44.62000
LogP 4.13
Vapour Pressure 0.0±0.8 mmHg at 25°C
Index of Refraction 1.524

 Synonyms

Methanimidamide, N'-(4-butyl-2-methylphenyl)-N-hydroxy-
N'-(4-Butyl-2-methylphenyl)-N-hydroxyimidoformamide
het0016
N-(4-butyl-2-methylphenyl)-N'-hydroxyiminoformamide
hms1445d06
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Price: ¥605/10 mM * 1 mL in DMSO

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