[CAS NO. 339068-25-6] HET0016
PRODUCTS SPECIFICATIONS [339068-25-6]
DESCRIPTION [339068-25-6]
Overview
| MDL | MFCD30719692 |
|---|---|
| Molecular Weight | 206.28 |
| Molecular Formula | C12H18N2O |
| SMILES | CCCCC1=CC=C(C(C)=C1)/N=C/NO |
1 Publications Citing Use of MCE
Summary
HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC 50 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] .
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]
.
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]
.
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. |
Appearance
Solid
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
DCM : 12.5 mg/mL ( 60.60 mM ; Need ultrasonic)
DMSO : 5 mg/mL ( 24.24 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 20% HP-β-CD in saline
Solubility: 2 mg/mL (9.70 mM); Clear solution; Need ultrasonic
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.