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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) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $29 | In Stock | |
5 mg | Inquiry | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $29 | In Stock |
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) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth. |
Targets&IC50 | CYP4A3: 20.6 nM , CYP4A2: 12.1 nM , CYP4A1:17.7 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 |
Smiles | CCCCc1ccc(N=CNO)c(C)c1 |
Relative Density. | 1.02g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DCM: 12.5 mg/mL (60.60 mM), Sonication is recommended. DMSO: 5 mg/mL (24.24 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/DCM
DCM
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