| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
CDK8 57 nM (IC50)
|
|---|---|
| ln Vitro |
CDK8-IN-15 has the highest anti-CDK8 activity, with an IC50 value of 57.3 nM, and has a positive effect on TNF-α-induced psoriasis in the HaCat cell model, with an IC50 value of 4.6 μM [1]. CDK8-IN-15 (5 μM, 4 h) inhibits CDK8 enzymatic activity and enhances the thermal stability of endogenous and exogenous CDK8 in HEK293T-CDK8 cells [1]. CDK8-IN-15 (0,1,2,4 μM, 75h) significantly reduces the levels of CXCL1, CXCL2, and IL-8 after treating HEK293 cells [1].
|
| ln Vivo |
CDK8-IN-15 (2 MG/KG, iv and 10 mg/kg, po) has high Caco-2 permeability in rats and has no significant inhibitory effect on the five cytochrome p450 isozymes [1]. CDK8-IN-15 does not cause significant tissue damage in ICE mice [1]. CDK8-IN-15 (5/10/20 MG/KG, po) may enhance IL-10 production and Foxp3 expression in IMQ-induced psoriasis model mice by targeting CDK8, thereby alleviating psoriasis [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HaCat Tested Concentrations: 0, 1 μM, 2 μM, 4 μM Incubation Duration: 75 h Experimental Results: Down-regulated the levels of IL-8 and IL-6 in a dose-dependent manner with values of 0, 1 μM, 2 μM, 4 μM . Western Blot Analysis[1] Cell Types: HEK293T-CDK8 Tested Concentrations: 5 μM Incubation Duration: 4 h Experimental Results: Enhanced the thermal stability of endogenous and exogenous CDK8. Western Blot Analysis[1] Cell Types: HEK 293 Tested Concentrations: 1 μM Incubation Duration: 0, 1, 2, 4, 8, 12 h. Experimental Results: Had a great NF-κB transcriptional activity inhibitory effect with an IC50 value of 1 μM. |
| Animal Protocol |
Animal/Disease Models: Rats[1]
Doses: 2 mg/kg, iv and 10 mg/kg, po Route of Administration: iv and po, a single administration Experimental Results: Showed high Caco-2 permeability in rats Animal/Disease Models: Imiquimod-induced psoriasis model of mice[1] Doses: 5, 10, 20 mg/kg Route of Administration: 5 % imiquimod cream and 5, 10, 20 mg/kg daily, p.o. Experimental Results: Alleviated the symptoms of imiquimod-induced psoriasis and increase the productions of TNF-α and IL-6 in imiquimod-induced psoriasis model of mice Animal/Disease Models: ICR mice[1]. Doses: 1000 mg/kg Route of Administration: i.g., a single administration Experimental Results: Didn’t cause a significant tissue damage on ICR mice |
| References |
| Molecular Formula |
C19H20N4O3
|
|---|---|
| Molecular Weight |
352.39
|
| CAS # |
2988020-03-5
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.8378 mL | 14.1888 mL | 28.3776 mL | |
| 5 mM | 0.5676 mL | 2.8378 mL | 5.6755 mL | |
| 10 mM | 0.2838 mL | 1.4189 mL | 2.8378 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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