| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 250mg | |||
| Other Sizes |
| Targets |
UKI-1 targets the urokinase-type plasminogen activator (uPA) system, which plays a critical role in extracellular matrix degradation, cell migration, and tumor invasion. The compound acts as a potent inhibitor of uPA with a Ki of 0.41 microM. By inhibiting uPA activity, UKI-1 blocks the activation of plasminogen to plasmin, thereby reducing extracellular matrix degradation and tumor cell invasion. This mechanism underlies its antimetastatic activity in preclinical cancer models.
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| ln Vitro |
Treatment with UKI-1 (WX-UK1; 0.1-1.0 μg/mL) showed a 50% reduction in tumor cells in a dual model of cervical cancer line HeLa and SCCHN line FaDu [1]. -UK1) prevents the plasminogen activating system from forming on two different levels: first, it prevents plasmin from forming directly, and second, it prevents plasmin from forming by inhibiting uPA. Effective inhibition of cell migration across the fibrin matrix by UKI-1 has been demonstrated in extrinsic models of highly intrinsic fibrosarcoma and breast cancer cells [1].
In vitro, UKI-1 is a potent inhibitor of the urokinase-type plasminogen activator system with a Ki of 0.41 microM. It inhibits the invasive capacity of carcinoma cells. As a low molecular weight serine protease inhibitor, UKI-1 effectively blocks uPA-mediated proteolysis. Its antimetastatic activity has been demonstrated in preclinical cancer models. These properties make UKI-1 a valuable tool for studying the role of the uPA system in cancer invasion and metastasis. |
| ln Vivo |
In metastatic pancreatic cancer and breast cancer models, UKI-1 (WX-UK1) therapy exhibits anti-metastatic efficacy and can dramatically reduce the number of metastases and tumor growth [1].
In vivo, UKI-1 has demonstrated potent antimetastatic activity in preclinical cancer models. By inhibiting the uPA system, the compound reduces tumor cell invasion and metastasis. Its efficacy in inhibiting the invasive capacity of carcinoma cells has been shown in various studies. UKI-1 is a potent antimetastatic agent. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile in different cancer models. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, UKI-1 is evaluated using enzymatic activity assays that measure uPA-mediated cleavage of chromogenic or fluorogenic substrates. The compound is incubated with recombinant uPA enzyme and substrate at various concentrations. uPA activity is quantified by measuring the release of chromophore or fluorophore. Ki values are determined from dose-response curves using appropriate kinetic models. Selectivity profiling against other serine proteases may be performed to confirm specificity. Standard assay conditions include physiological buffer systems with appropriate pH and ionic strength.
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| Cell Assay |
For in vitro cellular experiments, UKI-1 is tested in carcinoma cell lines to evaluate its effects on cell invasion and migration. Cells are cultured in appropriate media and treated with various concentrations of the compound. Cell invasion is assessed using Boyden chamber or Matrigel invasion assays. Cell migration is evaluated using wound healing or transwell migration assays. The compound's effects on cell viability, proliferation, and uPA activity are monitored using standard assays. The invasive capacity of carcinoma cells is quantified and compared to untreated controls.
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| Animal Protocol |
For in vivo animal experiments, UKI-1 can be administered to tumor-bearing mice via various routes including oral gavage, intravenous injection, or intraperitoneal injection, depending on its solubility and pharmacokinetic properties. The compound's antimetastatic efficacy can be evaluated in preclinical cancer models. Typical dosing regimens may range from 1 to 50 mg/kg. Tumor growth, metastasis formation, and survival are assessed. Pharmacodynamic markers such as uPA activity and plasmin generation are measured in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of UKI-1 are not extensively detailed in the public literature. As a small molecule with a molecular weight of 613.81, it may have reasonable bioavailability and tissue distribution. The compound is soluble in DMSO at ≥25 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies. The compound's metabolism and excretion pathways remain to be fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for UKI-1 are limited, as it is primarily a research tool. As a uPA inhibitor and serine protease inhibitor, its toxicity would depend on the importance of the uPA system for normal physiological processes such as tissue remodeling and wound healing. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References |
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| Additional Infomation |
WX-UK1 is a novel, non-cytotoxic small molecule based on 3-midinophenylalanine. In animal models, WX-UK1 blocks tumor cell invasion, metastasis, and primary tumor growth by inhibiting the serine protease and urokinase plasminogen activator (uPA) system. Studies have shown that the serine protease and urokinase plasminogen activator (uPA) system play a crucial role in the metastasis and primary tumor growth of breast cancer, gastric cancer, colon cancer, and various other solid tumors. Independent studies have demonstrated that administration of WX-UK1 reduces tumor cell invasiveness, suggesting its potential as adjuvant anti-metastatic therapy for cancer.
See also: WX-UK1 (note moved to). Drug Indications Studied for the treatment of solid tumors. Mechanism of Action Inhibits the uPA system by acting on the urokinase-type plasminogen activator receptor (uPAR). UKI-1 is a research compound used to study the uPA system and cancer metastasis. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a novel synthetic inhibitor of the uPA system with a Ki of 0.41 microM that inhibits the invasive capacity of carcinoma cells and is a potent antimetastatic agent. |
| Molecular Formula |
C32H47N5O5S
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|---|---|
| Molecular Weight |
613.8111
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| Exact Mass |
613.329
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| CAS # |
220355-63-5
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| PubChem CID |
9895193
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
745.5±70.0 °C at 760 mmHg
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| Flash Point |
404.6±35.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
6.36
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
43
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)N1CCN(CC1)C(=O)[C@H](CC2=CC(=CC=C2)C(=N)N)NS(=O)(=O)C3=C(C=C(C=C3C(C)C)C(C)C)C(C)C
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| InChi Key |
ISJSHQTWOHGCMM-NDEPHWFRSA-N
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| InChi Code |
InChI=1S/C32H47N5O5S/c1-8-42-32(39)37-14-12-36(13-15-37)31(38)28(17-23-10-9-11-24(16-23)30(33)34)35-43(40,41)29-26(21(4)5)18-25(20(2)3)19-27(29)22(6)7/h9-11,16,18-22,28,35H,8,12-15,17H2,1-7H3,(H3,33,34)/t28-/m0/s1
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| Chemical Name |
ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate
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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 : ~100 mg/mL (~162.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.07 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 25.0 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: ≥ 2.5 mg/mL (4.07 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 25.0 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: ≥ 2.5 mg/mL (4.07 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 | 1.6292 mL | 8.1458 mL | 16.2917 mL | |
| 5 mM | 0.3258 mL | 1.6292 mL | 3.2583 mL | |
| 10 mM | 0.1629 mL | 0.8146 mL | 1.6292 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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