| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
UCF-101 targets Omi/HtrA2, a mitochondrial serine protease that is released from the mitochondria in response to apoptotic stimuli. It is a selective and competitive inhibitor of this protease. Omi/HtrA2 is involved in the cellular response to stress and plays a role in the intrinsic pathway of apoptosis. By inhibiting Omi/HtrA2, UCF-101 can modulate apoptosis and other Omi/HtrA2-mediated processes.
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| ln Vitro |
MBP-Omi-(134-458)'s ability to modulate proteins is inhibited by Ucf-101 (20-100 μM; 30 min) [1]. His-Omi-(134-458) and β-casein test inhibition with His Ucf-101 (1-25 μM; 36 hours) The concentration adjustment approach inhibits His-Omi-(134-458) activity [1]. Ucf-101 (10-100 μM; 30 min) Adjust 10 min. Fibroblast cell disinfection that is dependent on caspase is negated by induction of the cytokine caspase-9 (-/-) [1]. At low doses (2.5 μM), Ucf-101 (1 – 20 μM; depletion in 1 hour) inhibits 6-OHDA-induced Parkinson’s disease (PD)–PC12 cells, while at high concentrations (≥10 μM), it increases cell fluorescence[3]. Ucf-101 (2.5 μM; sham 1 hour) Expression of C/EBP homologous protein (CHOP) and liposome regulatory protein 78 (Bip/Grp78) in PD-PC12 cells [3].
UCF-101 is a potent and selective inhibitor of Omi/HtrA2 with an IC50 of 9.5 μM for His-Omi. It shows very little activity against various other serine proteases, with IC50 values greater than 200 μM. This selectivity makes it a valuable tool for studying the specific role of Omi/HtrA2 in cellular processes. |
| ln Vivo |
Ucf-101 (0.6-1.8 μMol/kg; a single ip) reduces myocardial infarct size [2]. Ucf-101 (1.5 μMol/kg; a single ip) improves APO induction in an
UCF-101 has been shown to be effective in vivo. In a mouse model of spinal cord injury, it has been used to study the role of Omi/HtrA2. This suggests that the compound can cross the blood-brain barrier and exert its effects in the central nervous system. It is used to study the role of Omi/HtrA2 in various disease models. |
| Enzyme Assay |
The in vitro activity of UCF-101 is assessed using enzyme inhibition assays with purified recombinant Omi/HtrA2. The compound is incubated with the enzyme and a substrate, and the extent of inhibition is measured. The IC50 value of 9.5 μM for His-Omi is determined from these assays. Selectivity is confirmed by testing the compound against a panel of other serine proteases.
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| Cell Assay |
UCF-101's activity can also be studied in cell-based systems. In cells, its ability to inhibit Omi/HtrA2 can be assessed by measuring the activity of the protease or by monitoring downstream effects, such as the inhibition of apoptosis. Its effects on cellular responses to stress can also be evaluated.
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| Animal Protocol |
Animal/Disease Models: Myocardial ischemia/reperfusion (MI/R) injury in adult male mice (20-25 g) [1]
Doses: 0.6 spin behavior, increase positive cells and reverse the decrease of PD DA neurons [3]. , 1.5, 1.8 μmol/kg Route of Administration: intraperitoneal (ip) injection 10 minutes before reperfusion Experimental Results: Terminal dUTP nick end labeling staining, DNA ladder breakage incidence and infarct size reduction. UCF-101 has been evaluated in a mouse model of spinal cord injury. In these studies, the compound is typically administered to the animals, and its effects on functional recovery, tissue damage, and molecular markers of Omi/HtrA2 activity are assessed. The specific dosing and administration routes are not detailed in the provided excerpts. |
| ADME/Pharmacokinetics |
UCF-101 has a molecular weight of 495.51. Its chemical name is 5-((5-(2-nitrophenyl)furan-2-yl)methylene)-1,3-diphenyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione. It is a selective and competitive inhibitor of Omi/HtrA2. It is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
UCF-101 is a selective inhibitor of Omi/HtrA2 and its toxicity profile is not detailed in the provided sources. As an inhibitor of a pro-apoptotic protease, it could have effects on normal apoptotic processes. However, its high selectivity suggests that it may have a relatively favorable safety profile. In the mouse model of spinal cord injury, it was tolerated at the doses used.
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| References |
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| Additional Infomation |
UCF-101 (CAS#: 313649-08-0) is a selective and competitive inhibitor of the pro-apoptotic mitochondrial serine protease Omi/HtrA2 with an IC50 of 9.5 μM. It exhibits very little activity against various other serine proteases. UCF-101 is used as a research tool to study the role of Omi/HtrA2 in apoptosis and cellular stress responses. It has been evaluated in a mouse model of spinal cord injury.
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| Molecular Formula |
C27H17N3O5S
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|---|---|
| Molecular Weight |
495.5
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| Exact Mass |
497.104
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| CAS # |
313649-08-0
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| PubChem CID |
1102771
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| Appearance |
Orange to red solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
708.4±70.0 °C at 760 mmHg
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| Flash Point |
382.3±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.800
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| LogP |
5.07
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
36
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| Complexity |
864
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NVNSXBXKNMWKEJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H17N3O5S/c31-25-22(17-20-15-16-24(35-20)21-13-7-8-14-23(21)30(33)34)26(32)29(19-11-5-2-6-12-19)27(36)28(25)18-9-3-1-4-10-18/h1-17H
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| Chemical Name |
5-[[5-(2-nitrophenyl)furan-2-yl]methylidene]-1,3-diphenyl-2-sulfanylidene-1,3-diazinane-4,6-dione
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| Synonyms |
UCF101 UCF 101 UCF-101
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~25.23 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.79 mg/mL (3.61 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 1.67 mg/mL (3.37 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0182 mL | 10.0908 mL | 20.1816 mL | |
| 5 mM | 0.4036 mL | 2.0182 mL | 4.0363 mL | |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0182 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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