| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
CDK8-IN-15 (2 MG/KG, iv and 10 MG/KG , p.o.) shows high permeability and no obvious inhibition of the five cytochrome p450 isoenzymes [1].
CDK8-IN-15 (1000 MG/KG, i.g. ) doesn’t cause a significant tissue damage [1].
CDK8-IN-15 (5/10/20 MG/KG,i.g.) might enhance IL-10 production and Foxp3 expression by targeting CDK8, thereby alleviating psoriasis [1]. | Animal Model: | Rats[1] | | Dosage: | 2 mg/kg, iv and 10 mg/kg, po | | Administration: | iv and po, a single administration | | Result: | Showed high Caco-2 permeability in rats |
| Animal Model: | Imiquimod-induced psoriasis model of mice[1] | | Dosage: | 5, 10, 20 mg/kg | | Administration: | 5 % imiquimod cream and 5, 10, 20 mg/kg daily, p.o. | | 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 |
| Animal Model: | ICR mice[1]. | | Dosage: | 1000 mg/kg | | Administration: | i.g., a single administration | | Result: | Didn’t cause a significant tissue damage on ICR mice |
| [IC 50]
CDK8: 57 nM (IC50) | [References]
[1] Yan YY, et al.The discovery of a novel pyrrolo[2,3-b]pyridine as a selective CDK8 inhibitor offers a new approach against psoriasis[J]. 2024 May 6;175, 0753-3322. DOI:10.1016/j.biopha.2024.116705 |
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