| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
UK-122 targets urokinase-type plasminogen activator (uPA) with high selectivity. It has a Ki of 20 nM. The compound shows no or little inhibition of other serine proteases including thrombin, trypsin, plasmin, and tissue-type plasminogen activator, with IC50 values exceeding 100 μM. This high selectivity makes UK-122 a valuable tool for studying uPA function in cancer invasion and metastasis.
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| ln Vitro |
The invasiveness of CFPAC-1 cells is greatly reduced and cell migration is inhibited in a dose-dependent manner by UK122 (11.1, 33.3, 100 μM; 24 h) [1]. In CFPAC-1 cells, UK122 (10-100 μM; 48 hours) showed no influence on any changes in cell shape or growth [1].
UK-122 demonstrates potent and selective inhibition of uPA with an IC50 of 0.2 μM in cell-free indirect uPA assays. The compound shows negligible inhibition of tissue-type PA, plasmin, thrombin, and trypsin (all IC50 >100 μM). At 100 μM, UK-122 significantly suppresses cell migration on fibronectin-coated slides by 80% in pancreatic cancer CFPAC-1 cells. Importantly, it does not inhibit cancer cell growth, indicating its primary effect is on migration rather than proliferation. |
| ln Vivo |
In vivo activity data for UK-122 are not extensively detailed in the available literature. As an inhibitor of uPA, which plays a critical role in cancer cell invasion and metastasis, the compound would be expected to inhibit tumor dissemination and metastatic spread in vivo. Its ability to suppress cancer cell migration in vitro suggests potential for anti-metastatic activity in animal models. Specific in vivo efficacy data are not reported.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for UK-122 involve indirect uPA assays. The compound’s IC50 of 0.2 μM is determined in cell-free assays measuring uPA enzymatic activity. Selectivity is confirmed by testing against other serine proteases including thrombin, trypsin, plasmin, and tissue-type PA, with IC50 values >100 μM. Ki is determined to be 20 nM.
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| Cell Assay |
In vitro cell-based assays for UK-122 use pancreatic cancer CFPAC-1 cells. Cells are plated on fibronectin-coated slides and treated with UK-122 at 100 μM. Cell migration is assessed, and UK-122 suppresses migration by 80%. Cell growth is also monitored to confirm that the compound does not inhibit proliferation. These assays demonstrate the compound’s specific effect on cell migration without affecting cell viability.
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| Animal Protocol |
In vivo animal studies for UK-122 are not detailed in the available literature. As a uPA inhibitor with anti-migratory activity, typical in vivo evaluation would involve metastasis models where cancer cells are injected into mice and the compound’s ability to reduce metastatic spread is assessed. The compound’s lack of effect on cell growth suggests it would be evaluated primarily for anti-metastatic rather than anti-proliferative efficacy.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of UK-122 are not extensively reported. The compound has a molecular weight of 291.31 g/mol and a molecular formula of C17H13N3O2. It appears as a solid with a purity of >98% (HPLC). It is soluble at 10 mM in DMSO. Storage: powder at -20°C for 12 months or 4°C for 6 months; in solvent at -80°C for 6 months or -20°C for 6 months.
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| Toxicity/Toxicokinetics |
Specific toxicological data for UK-122 are not detailed in the available literature. The compound is classified for laboratory research use only and is not intended for human therapeutic use. As a uPA inhibitor, potential toxicities would relate to effects on plasminogen activation and tissue remodeling, though formal toxicological profiles are not reported.
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| References | |
| Additional Infomation |
UK-122 (CAS 940290-58-4) is a potent and selective inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 of 0.2 μM and a Ki of 20 nM. It shows negligible inhibition of thrombin, trypsin, plasmin, and tissue-type PA (IC50 >100 μM). At 100 μM, it suppresses pancreatic cancer cell migration by 80% without inhibiting cell growth. No clinical trial or approved indication data are available.
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| Molecular Formula |
C17H13N3O2
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|---|---|
| Molecular Weight |
291.304023504257
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| Exact Mass |
291.1
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| CAS # |
940290-58-4
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| Related CAS # |
940290-58-4 (free);1186653-73-5 (TFA salt);
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| PubChem CID |
16220264
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| Appearance |
White to yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C(=CC2C=CC(C(=N)N)=CC=2)N=C1C1C=CC=CC=1)=O
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| InChi Key |
JBHISGPWLXASFE-GXDHUFHOSA-N
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| InChi Code |
InChI=1S/C17H13N3O2/c18-15(19)12-8-6-11(7-9-12)10-14-17(21)22-16(20-14)13-4-2-1-3-5-13/h1-10H,(H3,18,19)/b14-10+
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| Chemical Name |
4-[(E)-(5-oxo-2-phenyl-1,3-oxazol-4-ylidene)methyl]benzenecarboximidamide
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~14.29 mg/mL (~49.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 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. Solubility in Formulation 2: ≥ 1.43 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 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. View More
Solubility in Formulation 3: ≥ 1.43 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4329 mL | 17.1644 mL | 34.3289 mL | |
| 5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL | |
| 10 mM | 0.3433 mL | 1.7164 mL | 3.4329 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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