| 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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| 250mg |
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| Targets |
EG1 targets the Paired box 2 (Pax2) transcription factor. It directly binds the paired domain of Pax2 with a Kd of 1.35-1.5 μM, blocking Pax2-DNA interaction and Pax2-mediated transcription. This inhibits Pax2 transcriptional activity without significant effects on Pax2 protein levels.
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| ln Vitro |
EG1 (0–12.5 μM; 48 hours) increases renal pelvic system activity while decreasing Pax2 [1]. Pax2-mediated EGFP expression can be inhibited by EG1 (0-500 μM), whereas Pax2 protein levels remain unaffected [1].
EG1 is a specific and efficacious inhibitor of Pax2-mediated transcription. It directly binds the paired domain of Pax2 (Kd=1.35-1.5 μM) and inhibits Pax2-DNA interactions. It can inhibit embryonic kidney development, a process directly dependent on Pax2 activity. It has no significant effects on Pax2 protein levels. |
| ln Vivo |
Specific in vivo activity data for EG1 is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of Pax2 inhibition and its impact on kidney development and cancer. It may be a good lead compound for developing tissue- and cell type-specific anticancer therapies.
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| Enzyme Assay |
EG1's activity as a Pax2 inhibitor is assessed using in vitro binding assays to measure its affinity for the Pax2 paired domain. Surface plasmon resonance (SPR) or other biophysical techniques can be used to determine the Kd of 1.35-1.5 μM. Its ability to inhibit Pax2-DNA interactions is assessed using electrophoretic mobility shift assays (EMSA) or DNA-binding assays.
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| Cell Assay |
Cell viability assay [1]
Cell Types: Pax2 positive: renal cell carcinoma cell line (RCC111), ovarian cancer cell line (TOV112D and ES-2); Pax2 negative: prostate cell line 22Rv1, PC3 or ovarian cancer cell line SK -OV-3 Tested Concentrations: 0, 12.5, 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: All Pax2-positive cells demonstrated a significant decrease in cell viability, while no Pax2-negative cells were affected. Cellular assays for EG1 involve treating cells with the compound and measuring Pax2-mediated transcription. Reporter gene assays, where cells are transfected with a Pax2-responsive luciferase reporter, are commonly used. The compound's effects on Pax2 target gene expression are assessed by qRT-PCR. |
| Animal Protocol |
In vivo animal model protocols for EG1 would involve its administration to animal models to study the role of Pax2 in development and cancer. Studies may include models of kidney development or Pax2-dependent cancers. The compound's effects on Pax2 activity and disease phenotypes would be assessed.
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| ADME/Pharmacokinetics |
EG1 has a molecular weight of 390.39. Specific pharmacokinetic data is not extensively detailed in the available literature. As a small molecule inhibitor, its pharmacokinetic properties would need to be evaluated in preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of EG1 has not been extensively characterized. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References |
[1]. Grimley E, et al. Inhibition of Pax2 Transcription Activation with a Small Molecule that Targets the DNA Binding Domain. ACS Chem Biol. 2017;12(3):724-734.
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| Additional Infomation |
EG1 (CAS# 693241-54-2) is a research compound used to study Pax2 function in development and cancer. It is a specific inhibitor of Pax2 transcription activation that targets the DNA binding domain. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C22H18N2O5
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|---|---|
| Molecular Weight |
390.395
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| Exact Mass |
390.121
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| CAS # |
693241-54-2
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| PubChem CID |
2193203
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
490.9±40.0 °C at 760 mmHg
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| Flash Point |
250.7±27.3 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.695
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| LogP |
3.98
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
588
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C1C=CC=CC=1C(NC1C=CC(C(NC2C=CC=CC=2C(=O)O)=O)=CC=1)=O
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| InChi Key |
GYZZRJRJYVMXNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18N2O5/c1-29-19-9-5-3-7-17(19)21(26)23-15-12-10-14(11-13-15)20(25)24-18-8-4-2-6-16(18)22(27)28/h2-13H,1H3,(H,23,26)(H,24,25)(H,27,28)
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| Chemical Name |
2-[[4-[(2-methoxybenzoyl)amino]benzoyl]amino]benzoic acid
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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 : ~83.33 mg/mL (~213.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.33 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 sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (5.33 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 20.8 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 | 2.5615 mL | 12.8074 mL | 25.6148 mL | |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.1230 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5615 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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