| UK 383367BMP-1/PCP inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | UK 383367 is a potent and selective inhibitor of BMP-1 with IC50 value of 44 nM. | |||||
| Targets | BMP-1 | |||||
| IC50 | 44 nM | |||||
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| Cas No. | 348622-88-8 | SDF | Download SDF |
| Synonyms | UK383367, UK-383367 | ||
| Chemical Name | 5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide | ||
| Canonical SMILES | C1CCC(CC1)CCCC(CC(=O)NO)C2=NC(=NO2)C(=O)N | ||
| Formula | C15H24N4O4 | M.Wt | 324.38 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
UK 383367 is a novel procollagen C-protein (PCP) inhibitor being investigated for the treatment of post-surgical dermal scarring, which potently inhibits the activity of PCP with the value of 50% inhibition concentration IC50 of 44 nM, as well as a selective inhibitor of matrix metalloproteinases (MMPs) with values of IC50 >60,000 nM for MMP-2 and >10,000 nM for MMP-1, MMP-3, MMP-9 and MMP-4. Although the mechanism is not clear yet, UK 383367 also exhibits weak inhibitory effects against phosphodiesterase-4 (PDE-4) enzyme, including PDE-4a, PDE-4b, PDE-4c and PDE-4d, with values of IC50 of 1.8 μM, 1.5 μM, 2.4 μM and 0.9 μM respectively.
Reference
G. A. Allan, J. I. Gedge, A. N. R. Nedderman, S. J. Roffey, H. F. Small and R. Webster. Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica 2006; 36(5): 399-418
Bailey S,Fish PV,Billotte S,Bordner J,Greiling D,James K,McElroy A,Mills JE,Reed C,Webster R.ff. Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. Bioorg Med Chem Lett.2008;18(24):6562-6567
