| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ML115 targets STAT3 (signal transducer and activator of transcription 3), a transcription factor that plays a critical role in cell proliferation, survival, angiogenesis, and immune regulation. Unlike most STAT3 modulators which are inhibitors, ML115 is a STAT3 agonist that activates STAT3 signaling. The compound is a molecular probe for signaling transducers and transcriptional activators. ML115 shows potent and selective activation of STAT3 with an EC₅₀ of 2.0 nM. The compound shows no activity against related STAT1 and NFκB, demonstrating excellent selectivity. By activating STAT3, ML115 enables researchers to study the effects of STAT3 activation on cellular processes and to investigate the role of STAT3 in cancer and other diseases.
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| ln Vitro |
In vitro studies have demonstrated that ML115 is a potent and selective STAT3 agonist with an EC₅₀ of 2.0 nM. The compound activates STAT3 signaling without affecting related STAT1 or NFκB pathways. In cell-based assays, ML115 treatment leads to STAT3 phosphorylation, nuclear translocation, and activation of STAT3 target gene expression. The compound's high potency (EC₅₀ = 2.0 nM) and selectivity make it a valuable tool for studying STAT3 function. ML115 has been used in studies of breast and prostate cancers, where STAT3 plays important roles in tumor progression and drug resistance. The compound's agonist activity enables researchers to study gain-of-function effects of STAT3 activation.
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| ln Vivo |
In vivo activity data for ML115 is limited in the available literature, as the compound is primarily used as a research tool in cell-based studies. The compound's potent STAT3 activation (EC₅₀ = 2.0 nM) suggests it could be useful for studying STAT3 function in vivo. However, comprehensive in vivo studies have not been extensively reported. The compound has been investigated for cancer research applications. Future studies may explore its effects in animal models to understand the role of STAT3 activation in tumor biology.
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| Enzyme Assay |
Cell-free biochemical assays for ML115 typically measure STAT3 activation or STAT3-DNA binding. A standard protocol involves incubating recombinant STAT3 protein with varying concentrations of ML115 (0.001-100 nM) and assessing STAT3 phosphorylation using kinase assays or using phospho-specific antibodies in ELISA format. STAT3-DNA binding activity can be measured using electrophoretic mobility shift assays (EMSA) or ELISA-based DNA binding assays with STAT3-specific DNA consensus sequences. EC₅₀ values are determined from dose-response curves using nonlinear regression analysis. Assays are performed in triplicate with appropriate positive and negative controls.
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| Cell Assay |
Cellular assays for ML115 typically use cell lines to assess STAT3 activation. A standard protocol involves culturing cells (e.g., breast or prostate cancer cell lines) in 96-well plates, treating with ML115 at concentrations ranging from 0.001-100 nM for 1-24 hours. STAT3 phosphorylation is assessed by Western blotting using phospho-specific antibodies (pSTAT3-Tyr705). STAT3 nuclear translocation is assessed by immunofluorescence microscopy or subcellular fractionation. STAT3 target gene expression (e.g., Bcl-2, Mcl-1, Cyclin D1) is measured by qPCR. Cell proliferation is assessed by MTT or CellTiter-Glo assays. The compound's selectivity for STAT3 over STAT1 and NFκB is confirmed by Western blotting for these pathways.
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| Animal Protocol |
In vivo studies with ML115 are limited, as the compound is primarily a research tool for in vitro applications. If conducted, a typical protocol might involve administration of ML115 to tumor-bearing mice by intraperitoneal or oral administration, followed by assessment of STAT3 phosphorylation and target gene expression in tumor tissues. However, comprehensive in vivo efficacy studies have not been extensively reported for this compound. Future studies may explore its effects in animal models to understand the role of STAT3 activation in cancer and other diseases.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ML115 is limited, as the compound is primarily used in research settings. The compound's molecular weight is 322.74 g/mol. The compound's physicochemical properties suggest moderate polarity. For in vivo applications, the compound would likely require formulation to enhance bioavailability. The compound is typically dissolved in DMSO for in vitro studies. Metabolism and clearance pathways have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Toxicological data specific to ML115 is limited, as the compound is a research chemical used primarily in in vitro settings. At effective concentrations (2.0 nM for STAT3 activation), the compound does not show significant cytotoxicity in most cell types. Higher concentrations may have off-target effects or cytotoxicity. As a STAT3 agonist, potential effects could arise from activation of STAT3 in tissues where the pathway is important for normal function. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
N-(4-chloro-2,5-dimethoxyphenyl)-5-cyclopropyl-3-isoxazolecarboxamide is an aromatic amide.
ML115 is a research compound and not an approved drug. No clinical trials or regulatory approvals exist for this compound. It is commercially available from various suppliers for research use only. The compound's primary value lies in its utility as a pharmacological tool for studying STAT3 function. With an EC₅₀ of 2.0 nM for STAT3 activation and no activity against STAT1 or NFκB, ML115 is a highly potent and selective STAT3 agonist that enables researchers to investigate the roles of STAT3 signaling in cancer, cell proliferation, and other biological processes. As an agonist rather than an inhibitor, ML115 provides a unique tool for studying gain-of-function effects of STAT3 activation. |
| Molecular Formula |
C15H15CLN2O4
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|---|---|
| Molecular Weight |
322.74
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| Exact Mass |
322.072
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| CAS # |
912798-42-6
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| PubChem CID |
6619100
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
422.9±45.0 °C at 760 mmHg
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| Flash Point |
209.6±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
2.61
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
407
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=C(C=C1NC(=O)C2=NOC(=C2)C3CC3)OC)Cl
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| InChi Key |
FMWABCRYNLCXOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15ClN2O4/c1-20-13-6-10(14(21-2)5-9(13)16)17-15(19)11-7-12(22-18-11)8-3-4-8/h5-8H,3-4H2,1-2H3,(H,17,19)
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| Chemical Name |
N-(4-chloro-2,5-dimethoxyphenyl)-5-cyclopropyl-1,2-oxazole-3-carboxamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 20 mg/mL (61.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0985 mL | 15.4923 mL | 30.9847 mL | |
| 5 mM | 0.6197 mL | 3.0985 mL | 6.1969 mL | |
| 10 mM | 0.3098 mL | 1.5492 mL | 3.0985 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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