| CAS NO: | 313649-08-0 |
| 包装 | 价格(元) |
| 10mM 1 mL in DMSO | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Cas No. | 313649-08-0 |
| 化学名 | 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=C\C3=CC=C(C4=CC=CC=C4[N+]([O-])=O)O3)=O)N(C5=CC=CC=C5)C2=O |
| 分子式 | C27H17N3O5S |
| 分子量 | 495.5 |
| 溶解度 | ≤5mg/ml in DMSO;20mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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