2. Cell Cycle/DNA Damage
  3. CDK
  4. 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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CDK8-IN-15 Chemical Structure

CDK8-IN-15 Chemical Structure

CAS No. : 2988020-03-5

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CDK8-IN-15 Related Antibodies

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Description

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].
IC50 & Target[1]

CDK8

57 nM (IC50)

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.

CDK8-IN-15 Related Antibodies

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
Molecular Weight

352.39

Formula

C19H20N4O3
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK8-IN-15 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK8-IN-152988020-03-5CDKCyclin dependent kinaseHaCat cellsTNF-α-induced psoriasis model of miceinflammatory responseICR micethermal stabilitypsoriasis diseasesInhibitorinhibitorinhibit

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