CDK8-IN-15
CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases.
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- CAS No.: 2988020-03-5
- Formule: C19H20N4O3
- Masse moléculaire:352.39
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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CDK8 57 nM (IC50) |
CDK8-IN-15 exhibits the highest activity against CDK8 with an IC50 value of 57.3 nM and exerts a positive effect on the TNF-α-induced psoriasis model of HaCat cells with an IC50 value of 4.6 μM [1]. CDK8-IN-15 (5 μM, 4 h) inhibits CDK8 enzyme 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, IL-8 in HEK293 cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCat cells
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Concentration:0, 1 μM, 2 μM, 4 μM
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Incubation Time:75 h
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Result: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 .
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Cell Line:HEK293T-CDK8 cells
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Concentration:5 μM
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Incubation Time:4 h
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Result:Enhanced the thermal stability of endogenous and exogenous CDK8.
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Cell Line:HEK 293 cells
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Concentration:1 μM
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Incubation Time:0, 1, 2, 4, 8, 12 h.
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Result:Had a great NF-κB transcriptional activity inhibitory effect with an IC50 value of 1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:2 mg/kg, iv and 10 mg/kg, po
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Administration:iv and po, a single administration
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Result:Showed high Caco-2 permeability in rats
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Animal Model:Imiquimod-induced psoriasis model of mice[1]
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Dosage:5, 10, 20 mg/kg
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Administration:5 % imiquimod cream and 5, 10, 20 mg/kg daily, p.o.
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Result:Alleviated the symptoms of imiquimod-induced psoriasis and increase the productions of TNF-α and IL-6 in imiquimod-induced psoriasis model of mice
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Animal Model:ICR mice[1].
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Dosage:1000 mg/kg
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Administration:i.g., a single administration
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Result:Didn’t cause a significant tissue damage on ICR mice
Chemical Information
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CAS No. 2988020-03-5
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Masse moléculaire 352.39
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Formule C19H20N4O3
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SMILES
O=C(NC1=CC(OC)=C(C2=CC(C=CN3)=C3N=C2)C=C1)N4CCOCC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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