| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
EED-IN-4 (compound 19) (5 μM; 24 h) reduced the level of H3K27me3 in DC2.4 cells by 79.94% and inhibited CCL19/CCL21-induced cell migration [1]. EED-IN-4 had a weak inhibitory effect on hERG channel currents in stably transfected HEK293T cells, with an IC50 > 10 μM [1]. EED-IN-4 was much more selective for EED than for the methyltransferase activity of EZH2 [1]. EED-IN-4 was negative in the Mini-Ames mutagenicity assay containing Salmonella Typhimurium TA100 [1].
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| ln Vivo |
EED-IN-4 (compound 19) (40-80 mg/kg; orally; twice daily; day 9 to day 30 post-immunization) dose-dependently alleviated clinical symptoms in female C57BL/6 mouse models of experimental autoimmune encephalomyelitis (EAE), reduced the degree of spinal cord inflammation infiltration, and inhibited the activation and infiltration of dendritic cells, macrophages, and pathogenic T cells in peripheral lymph nodes and the central nervous system [1]. EED-IN-4 (100 mg/kg; orally; twice daily; for 30 consecutive days) did not show significant acute or subacute toxicity in C57BL/6 mouse models (equal number of male and female mice). Mice had normal weight gain, no significant abnormalities in blood routine tests, liver and kidney function indicators, and no histopathological damage was observed in major organs including the heart, liver, spleen, lungs, and kidneys [1]. EED-IN-4 (80 mg/kg; intragastric administration (ig); single dose) preferentially and persistently accumulates in key immune lymph nodes of healthy female C57BL/6 mice, including axillary, inguinal and cervical lymph nodes, at concentrations significantly higher than EED226, demonstrating good lymphotropic behavior [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: DC2.4 Dendritic Cells Tested Concentrations: 5 μM Incubation Duration: 24 hours Experimental Results: Compared with the control group, the H3K27me3 protein level in DC2.4 cells decreased by 79.94%. Cell migration assay [1] Cell Types: DC2.4 dendritic cells Tested Concentrations: 5 μM Incubation Duration: 24 hours (pretreatment); 12 hours (migration assay) Experimental Results: Inhibited CCL19/CCL21-induced DC2.4 cell migration by 60.64%, which was 1.6 times more potent than the positive control EED226. |
| Animal Protocol |
Animal/Disease Models:Eight-week-old female C57BL/6 mice, experimental autoimmune encephalomyelitis (EAE) model [1]
Doses: 40 mg/kg, 80 mg/kg Route of Administration: Oral; twice daily; from day 9 to day 30 post-immunization Experimental Results: Dose-dependently reduced disease susceptibility and alleviated clinical symptoms throughout the disease course. It significantly inhibited inflammatory cell infiltration in the spinal cord and reduced the proportion of total CD11c+ dendritic cells, mature dendritic cells (CD11c+CD80+ or CD11c+MHC-II+), F4/80+CD11b+ macrophages, F4/80+CD80+ inflammatory macrophages, and pro-inflammatory Th1 (CD4+IFN-γ+) and Th17 (CD4+IL-17+) T cells in peripheral lymph nodes. In addition, it reduced the infiltration of CD11c+ dendritic cells, CD11b+ macrophages and CD4+ T cells into the spinal cord and brain of EAE mice. |
| References |
| Molecular Formula |
C22H20FN5O
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|---|---|
| Molecular Weight |
389.43
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CN(C)C1=CC=C(C2=CN=C(NCC3=C(F)C=CC4=C3CCO4)C=C2C#N)C=N1
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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 | 2.5679 mL | 12.8393 mL | 25.6786 mL | |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1357 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5679 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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