IF 12
PMID: 38389848 ↗HET0016
Catalog No.: GC11540Purity:>98.50%Synonyms: N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine
HET0016 is a highly selective inhibitor of 20-hydroxy eicosatrienoic acid (20-HETE) synthase. The IC50 values for the catalytic synthesis of 20-HETE by recombinant CYP4A1, CYP4A2, and CYP4A3 are 17.7nM, 12.1nM, and 20.6nM, respectively.
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Cas No.: 339068-25-6
10mM (in 1mL DMSO)In Stock
$55.00
1
1mgIn Stock
$23.00
1
5mgIn Stock
$50.00
1
10mgIn Stock
$86.00
1
25mgIn Stock
$171.00
1
50mgIn Stock
$315.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $55.00 | In Stock | 1 | |
| 1mg | $23.00 | In Stock | 1 | |
| 5mg | $50.00 | In Stock | 1 | |
| 10mg | $86.00 | In Stock | 1 | |
| 25mg | $171.00 | In Stock | 1 | |
| 50mg | $315.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
HET0016 is a highly selective inhibitor of 20-hydroxy eicosatrienoic acid (20-HETE) synthase. The IC50 values for the catalytic synthesis of 20-HETE by recombinant CYP4A1, CYP4A2, and CYP4A3 are 17.7nM, 12.1nM, and 20.6nM, respectively [1-2]. 20-HETE is an effective vasoconstrictor that can inhibit Na+ transport in the proximal tubule and thick ascending limb of the loop of Henle (TALH) [3]. HET0016 can be used to inhibit angiogenesis and tumor growth [4].
In vitro, treatment with HET0016 (100μM; 24, 48h) significantly reduced the motility of 4T1 and MDA-MB-231 cells, the total area of cell invasion decreased, and cell migration also showed a similar reduction [4]. Treatment with HET0016 (1, 10μM; 48h) dose-dependently inhibited the cell proliferation of the 9L gliosarcoma cell line. HET0016 could inhibit proliferation induced by epidermal growth factor (EGF) and platelet-derived growth factor (PDGF) and reduce the phosphorylation of PDGF receptors [5].
In vivo, HET0016 (10mg/kg/day; 5d; i.p.) Treatment reduced tumor growth in breast cancer xenograft model mice, and decreased tumor volume in both the early treatment group and the delayed treatment group [6]. HET0016 (10mg/kg/day; once every 12 hours for three days; i.p.) treatment significantly reduced the brain lesion volume and neurological deficits in collagenase-induced Intracerebral Hemorrhage (ICH) model mice, and decreased neuronal death, ROS production, gelatin dissolution activity and inflammatory response 3 days after ICH [7].
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 T F, Zuccari D A P C, Jardim-Perassi B V, et al. HET0016, a selective inhibitor of 20-HETE synthesis, decreases pro-angiogenic factors and inhibits growth of triple negative breast cancer in mice[J]. PLoS One, 2014, 9(12): e116247.
[3] Hoagland K M, Flasch A K, Roman R J. Inhibitors of 20-HETE formation promote salt-sensitive hypertension in rats[J]. Hypertension, 2003, 42(4): 669-673.
[4] Borin TF, et al. HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model. PLoS One. 2017 Jun 13;12(6): e0178830.
[5] Guo M, Roman R J, Fenstermacher J D, et al. 9L gliosarcoma cell proliferation and tumor growth in rats are suppressed by N-hydroxy-N′-(4-butyl-2-methylphenol) formamidine (HET0016), a selective inhibitor of CYP4A[J]. The Journal of pharmacology and experimental therapeutics, 2006, 317(1): 97-108.
[6] Borin T F, Zuccari D A P C, Jardim-Perassi B V, et al. HET0016, a selective inhibitor of 20-HETE synthesis, decreases pro-angiogenic factors and inhibits growth of triple negative breast cancer in mice[J]. PLoS One, 2014, 9(12): e116247.
[7] Han X, Zhao X, Lan X, et al. 20-HETE synthesis inhibition promotes cerebral protection after intracerebral hemorrhage without inhibiting angiogenesis. J Cereb Blood Flow Metab. 2019;39(8):1531-1543.
Protocol
| Cell experiment [1]: | |
Cell lines | 4T1 luciferase positive cells and MDA-MB-231 cells |
Preparation Method | Wound healing assay was performed to detect the potential of HET0016 treatment to decrease migration malignant cells. 4T1 luciferase positive cells and MDA-MB-231 cells achieving 80-90% of confluency in 6 well plates were starved overnight with 0.5% FBS for cell cycle synchronization. Then, cells were treated with 100μM of HET0016 for 24 and 48 hours in 2% FBS media, and microphotographed every 24 hours. The wound size was measured using Image J software (NIH) by drawing a rectangular region of interest to quantify the visible area of wound. |
Reaction Conditions | 100μM; 24 and 48h |
Applications | HET0016 significantly reduced the motility of 4T1 luciferase positive cells and MDA-MB-231 cells, the total area of cell invasion decreased, and cell migration also showed a similar reduction. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice |
Preparation Method | Athymic nude female mice (n = 28) 6–8 week-old and weighing 20–25 grams obtained from Charles River laboratory (Frederick, MD) were used in all experiments. After tumor implantation the animals received treatment with HET0016 (10mg/kg per day) or phosphate buffered saline (PBS) containing 10% of dimethyl sulfoxide (DMSO) and 10% cremophor as a vehicle control intraperitoneally (IP) for five days during the week (Monday through Friday). To better evaluate the effect of treatment, the animals were divided into four treatment groups receiving early treatment (beginning on the day of tumor inoculation) or delayed (on day 8 after inoculation of the tumor) and maintained for 21 or 28 days. Group 1 (n = 6) starting treatment early on day 0 until day 21; Group 2 (n = 4) also starting treatment early on day 0, however, was maintained for 28 days; Group 3 (n = 6) starting treatment delayed, after tumor establishment on day 8 until day 21 and Group 4 (n = 4) also starting treatment delayed on day 8, however, was maintained for 28 days. Eight animals were used as control receiving vehicle, four were maintained for 21 days and others four were maintained for 28 days. |
Dosage form | 10mg/kg/day for 5 days; i.p. |
Applications | HET0016 treatment decreased tumor volume in all animals in both early and delayed treatment groups. |
References: | |
Product Documents
Purity:>98.50%Appearance:A solid
Biological Data
1 / 1
Chemical Properties
CAS No.
339068-25-6
Synonyms
N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine
Chemical Name
N-(4-butyl-2-methylphenyl)-N'-hydroxy-methanimidamide
SMILES
CCCCC1=CC=C(/N=C/NO)C(C)=C1
Molecular Formula
C12H18N2O
Molecular Weight
206.3
Solubility
≤14mg/ml in ethanol;14mg/ml in DMSO;14mg/ml in dimethyl formamide
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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