1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK8-IN-9

CDK8-IN-9 

Cat. No.: HY-151255
Handling Instructions

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.

For research use only. We do not sell to patients.

CDK8-IN-9 Chemical Structure

CDK8-IN-9 Chemical Structure

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Description

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies[1].

In Vitro

CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF[1].
CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis[1].

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

Cell Viability Assay[1]

Cell Line: HCT-116, HT-29, SW-480, CT-26 and GES-1 cells
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Inhibited HCT-116, HT-29, SW-480, CT-26 and GES-1 cells with the GI50 values of 4.9, 4.3, 2.1, 4.0 and 61.5 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1, and 2 μM
Incubation Time: 24 hours
Result: Arrested cells in G2/M phase by 17%, 20.26% and 34.45% at concentrations of 0.5, 1, and 2 μM, respectively.
Showed a decrease in the G0/G1 phase and a slight increase in the S phase.
In Vivo

CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells[1].

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

Animal Model: Sprague−Dawley rats[1]
Dosage: 10 mg/kg or 5 mg/kg
Administration: p.o. for 10 mg/kg and i.v. for 5 mg/kg
Result: The pharmacokinetic parameters of CDK8-IN-9 (compound 22)
Parameters t1/2 (h) Tmax (h) MRT (h) Cmax (μg/L) AUC0-∞ (μg/L·h) CL (L/h/kg) F (%)
10 mg/kg (po) 1.21 0.75 2.022 497.56 783.66 9.23 39.8
5 mg/kg (iv) 1.63 - 1.756 706.29 983.09 11.32 -
Molecular Weight

423.43

Formula

C24H20F3N3O

SMILES

O=C(NC1=CC=C(C)C(C(F)(F)F)=C1)CCC2=CC=CC(C3=CN=C(NC=C4)C4=C3)=C2

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
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CDK8-IN-9
Cat. No.:
HY-151255
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