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.
Product information
CAS Number: 339068-25-6
Molecular Weight: 206.28
Formula: C12H18N2O
Chemical Name: (E)-N'-(4-butyl-2-methylphenyl)-N-hydroxymethanimidamide
Smiles: CC1=CC(CCCC)=CC=C1/N=C/NO
InChiKey: LYNOGBKNFIHKLE-UHFFFAOYSA-N
InChi: InChI=1S/C12H18N2O/c1-3-4-5-11-6-7-12(10(2)8-11)13-9-14-15/h6-9,15H,3-5H2,1-2H3,(H,13,14)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (24.24 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A . HET0016 (100 μM; 24 hours, 48 hours) decreases 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. HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice. 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.
Products are for research use only. Not for human use.
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