UCF 101

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UCF 101

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

313649-08-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	495.5
Cas No.	313649-08-0
Formula	C₂₇H₁₇N₃O₅S
Solubility	≤5mg/ml in DMSO;20mg/ml in dimethyl formamide
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=C\C3=CC=C(C4=CC=CC=C4[N+]([O-])=O)O3)=O)N(C5=CC=CC=C5)C2=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).