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2988020-03-5

2988020-03-5 Structure

2988020-03-5 Structure
IdentificationBack Directory
[Name]

CDK8-IN-15
[CAS]

2988020-03-5
[Synonyms]

CDK8-IN-15
[Molecular Formula]

C19H20N4O3
[MOL File]

2988020-03-5.mol
[Molecular Weight]

352.39
Chemical PropertiesBack Directory
[density ]

1.344±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[pka]

12.76±0.70(predicted)
Hazard InformationBack 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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