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Art. -Nr.: HY-162600

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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. Nr.: 2988020-03-5
Formel: C₁₉H₂₀N₄O₃
Molecular Weight:352.39

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

CDK8-IN-15 Chemical Structure

CAS. Nr.: 2988020-03-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK8

57 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

HaCat cells
Concentration:

0, 1 μM, 2 μM, 4 μM
Incubation Time:

75 h
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 .

Western Blot Analysis^[1]

Cell Line:

HEK293T-CDK8 cells
Concentration:

5 μM
Incubation Time:

4 h
Result:

Enhanced the thermal stability of endogenous and exogenous CDK8.

Western Blot Analysis^[1]

Cell Line:

HEK 293 cells
Concentration:

1 μM
Incubation Time:

0, 1, 2, 4, 8, 12 h.
Result:

Had a great NF-κB transcriptional activity inhibitory effect with an IC₅₀ value of 1 μM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Chemical Information

CAS. Nr. 2988020-03-5
Molecular Weight 352.39
Formel C₁₉H₂₀N₄O₃
SMILES

O=C(NC1=CC(OC)=C(C2=CC(C=CN3)=C3N=C2)C=C1)N4CCOCC4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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CDK8-IN-15

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CDK8-IN-15 Related Classifications

HY-162600 Related Classifications