| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Cdc25A, Cdc25B, Cdc25C phosphatases. JUN-1111 also inhibits the dual-specificity phosphatase VHR and the protein tyrosine phosphatase PTP1B with lower potency. It is a selective inhibitor with irreversible binding mechanism.
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|---|---|
| ln Vitro |
In tsFT210 cells, JUN-1111 (10, 30 µM; 17 h) stimulates cell cycle marketing in the G1 and G2/M phases [1]. Reactive oxygen species production in cells is induced by JUN-1111 (10, 30 µM; 1 h) in a way akin to lowering tsFT210 JUN-1111 (0-20 µM) [2].
JUN-1111 shows IC50 values of 0.38 µM for Cdc25A, 1.8 µM for Cdc25B, 0.66 µM for Cdc25C, 28 µM for VHR, and 37 µM for PTP1B. The compound demonstrates potent inhibition against Cdc25A and Cdc25C with sub-micromolar IC50 values, while showing significantly lower potency against VHR and PTP1B, indicating selectivity for the Cdc25 family phosphatases. |
| ln Vivo |
No detailed in vivo activity data has been published in the available literature. JUN-1111 is primarily characterized as a biochemical tool for studying Cdc25 phosphatase function in cell cycle regulation. Further in vivo studies would be needed to evaluate its pharmacokinetic and pharmacodynamic properties in animal models.
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| Enzyme Assay |
Cdc25 phosphatase activity assay: Recombinant Cdc25A, Cdc25B, or Cdc25C is incubated with varying concentrations of JUN-1111 and the fluorogenic substrate 3-O-methylfluorescein phosphate (OMFP) in assay buffer (50 mM Tris-HCl, pH 8.0, 50 mM NaCl, 1 mM DTT, 0.1 mg/mL BSA) at 37°C for 30-60 min. The fluorescence intensity of the product (3-O-methylfluorescein) is measured at excitation 485 nm and emission 525 nm. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: tsFT210 cells Tested Concentrations: 10, 30 µM Incubation Duration: 17 hrs (hours) Experimental Results: Induced cell cycle arrest in G1 and G2/M phases. Western Blot Analysis[1] Cell Types: tsFT210 Cell Tested Concentrations: 10, 30 µM Incubation Duration: 1 hour Experimental Results: diminished the expression of phosphorylated Cdk1 in a dose-dependent manner. Cell cycle analysis: Cancer cells (e.g., HeLa or MCF-7) are treated with JUN-1111 at varying concentrations (0.1-10 µM) for 24-48 hours. Cells are harvested, fixed with 70% ethanol, stained with propidium iodide, and analyzed by flow cytometry to determine cell cycle distribution. The percentage of cells in G1, S, and G2/M phases is quantified. Phospho-Cdk1 expression is assessed by Western blot. |
| Animal Protocol |
No in vivo animal experimental protocols have been published for JUN-1111 in the available literature. As a research tool for cell cycle studies, in vivo applications would typically involve xenograft tumor models in immunocompromised mice, with compound administration by intraperitoneal or oral routes, followed by tumor volume measurement and histopathological analysis.
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been published in the available literature. JUN-1111 has a molecular weight of 287.31 g/mol and is typically stored at -20°C. Stock solutions are prepared in DMSO. Comprehensive PK parameters such as bioavailability, half-life, and plasma protein binding remain to be characterized.
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| Toxicity/Toxicokinetics |
No toxicity data has been published in the available literature. JUN-1111 is for research use only and not for human use. Standard laboratory safety practices should be followed when handling this compound, including the use of personal protective equipment and proper waste disposal.
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| References | |
| Additional Infomation |
JUN-1111 is an irreversible, selective Cdc25 phosphatase inhibitor. Cdc25 phosphatases are key regulators of cell cycle progression by dephosphorylating and activating cyclin-dependent kinases (Cdks). Inhibition of Cdc25 leads to cell cycle arrest at G1 and G2/M checkpoints. JUN-1111 reduces phospho-Cdk1 expression, consistent with Cdc25 inhibition. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C15H17N3O3
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|---|---|
| Molecular Weight |
287.31
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| Exact Mass |
287.127
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| CAS # |
874351-38-9
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| Related CAS # |
NSC668394;382605-72-3
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| PubChem CID |
11392050
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| Appearance |
Orange to reddish brown solid powder
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| LogP |
0.595
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
443
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QWIRJCMQNFHGJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17N3O3/c19-13-10-12(15(20)14-11(13)2-1-3-17-14)16-4-5-18-6-8-21-9-7-18/h1-3,10,16H,4-9H2
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| Chemical Name |
7-(2-morpholin-4-ylethylamino)quinoline-5,8-dione
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| Synonyms |
JUN1111; JUN 1111; JUN-1111
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4806 mL | 17.4028 mL | 34.8056 mL | |
| 5 mM | 0.6961 mL | 3.4806 mL | 6.9611 mL | |
| 10 mM | 0.3481 mL | 1.7403 mL | 3.4806 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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