UCF 101 |
Catalog No.GC13421
One-Click Copy Product Info
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inhibitor of the proteolytic activity of Omi/HtrA2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 313649-08-0
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 313649-08-0 | 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=C\C3=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 |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0182 mL | 10.0908 mL | 20.1816 mL |
| 5 mM | 403.6 μL | 2.0182 mL | 4.0363 mL |
| 10 mM | 201.8 μL | 1.0091 mL | 2.0182 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A crystalline solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)