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Chemical Structure : HET0016
CAS No.: 339068-25-6
Catalog No.: PC-35319Not For Human Use, Lab Use Only.
HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.
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|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $258 | In stock | |
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HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.
HET0016 inhibits 20-HETE formation in rat renal microsomes with IC50 of 35 nM, shows no significant inhibition of the formation of epoxyeicosatrienoic acids (IC50=2,800 nM).
HET0016 also inhibits the CYP2C9, CYP2D6 and CYP3A4-catalysed substrates oxidation at higher concentrations (IC50=3,300, 83,900 and 71,000 nM).
HET0016 reduces protein tyrosine and p42/p44 MAPK phosphorylation, significantly inhibits the U251 proliferation and phosphorylation of both the EGFR and p42/p44 MAPK induced by EGF.
HET0016 suppresses 9L gliosarcoma cell proliferation and tumor growth in rats.
| M.Wt | 206.289 | |
| Formula | C12H18N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(4-butyl-2-methylphenyl)-N'-hydroxy-methanimidamide |
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1. Sato M, et al. Bioorg Med Chem Lett. 2001 Dec 3;11(23):2993-5.
2. Guo M, et al. J Pharmacol Exp Ther. 2005 Nov;315(2):526-33.
3. Miyata N, et al. Br J Pharmacol. 2001 Jun;133(3):325-9.
4. Guo M, et al. J Pharmacol Exp Ther. 2006 Apr;317(1):97-108.
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