| UCF 101inhibitor of the proteolytic activity of Omi/HtrA2 |
Sample solution is provided at 25 µL, 10mM.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 313649-08-0 | SDF | Download SDF |
| Chemical Name | dihydro-5-[[5-(2-nitrophenyl)-2-furanyl]methylene]-1,3-diphenyl-2-thioxo-4,6(1H,5H)-pyrimidinedione | ||
| Canonical SMILES | S=C(N(C1=CC=CC=C1)C(/C2=CC3=CC=C(C4=CC=CC=C4[N+]([O-])=O)O3)=O)N(C5=CC=CC=C5)C2=O | ||
| Formula | C27H17N3O5S | M.Wt | 495.5 |
| Solubility | ≤5mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline 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. | ||
IC50: 9.5 μM
UCF 101 is an inhibitor of Omi/HtrA2.
Omi/HtrA2, a mitochondria serine protease with close homology to bacterial HtrA chaperones, is released from the mitochondria in response to apoptotic stimuli. Omi/HtrA2 has been reported to be able to induce cell death via a mechanism involving its protease activity.
In vitro: UCF 101 was identified in a HTS of a combinatorial library using Omi-(134-458) protease and fluorescein-casein as a generic substrate. UCF 101 exhibited specific activity against Omi/HtrA2 and very little activity against other serine proteases. UCF 101 showed a natural fluorescence that was used to monitor its ability to enter mammalian cells. In addition, when tested in caspase-9 (-/-) null fibroblasts, UCF 101 was able to inhibit Omi/HtrA2-induced cell death [1].
In vivo: In a previous study, rats were intraperitoneally administered UCF-101 at 1.5 micromol/kg 10 min prior to reperfusion. Results showed that UCF-101 treatment could significantly decrease cerebral infarct size by about 16.27% and also improve neurological behavior. Moreover, UCF-101 treatment was able to reduce TUNEL-positive cells in the cerebral cortex significantly. In addition, the upregulation in the expression of FasL and the cleavage products of active caspase-3 and caspase-8 induced by ischemia was attenuated in mice treated with UCF-101, while upregulation of FLIP levels was increased [2].
Clinical trial: So far, no clinical study has been conducted.
References:[1] Cilenti, L.,Lee, Y.,Hess, S., et al. Characterization of a novel and specific inhibitor for the pro-apoptotic protease Omi/HtrA2. The Journal of Biological Chemisty 278(13), 11489-11494 (2003).[2] Su, D.,Su, Z.,Wang, J., et al. UCF-101, a novel Omi/HtrA2 inhibitor, protects against cerebral ischemia/reperfusion injury in rats. Anat.Rec.(Hoboken) 292(6), 854-861 (2009).
