2. Cell Cycle/DNA Damage Stem Cell/Wnt
  3. CDK β-catenin
  4. CDK8-IN-11

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.

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

CDK8-IN-11 Chemical Structure

CDK8-IN-11 Chemical Structure

CAS No. : 2839338-28-0

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Based on 1 publication(s) in Google Scholar

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CDK8-IN-11 Related Antibodies

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Description

CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer[1].

IC50 & Target[1]

CDK8

46 nM (IC50)

In Vitro

CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% [1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) reverses Sorafenib (HY-10201) resistance of HCT-116 cells[1].

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

CDK8-IN-11 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT-116, HHT-29, SW480, CT-26, GES-1 cells
Concentration: 0.08, 0.4, 2, 10, and 50 μM
Incubation Time: 48 h
Result: Inhibited cell proliferation with IC50 values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.

Western Blot Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0, 1, 2, 4 μM
Incubation Time: 48 h
Result: Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cell
Concentration: 0.5-2 μM
Incubation Time: 48 h
Result: Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells.
In Vivo

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10−6 cm/s[1].

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

Animal Model: CT-26 xenograft mice[1]
Dosage: 10 and 40 mg/kg
Administration: Oral adminstration (p.o.)
Result: Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Animal Model: Rats (pharmacokinetic assay)[1]
Dosage: 10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration: Oral adminstration (p.o.) or intravenous injection (i.v.)
Result: Pharmacokinetic profile of CDK8-IN-11 (compound 29).
dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) F (%)
10 (p.o.) 1.1 0.8 453 31.7
2 (i.v.) 0.5 318
Molecular Weight

388.34

Formula

C19H15F3N4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(OC3=CC=C(N)N=C3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (643.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5751 mL 12.8753 mL 25.7506 mL
5 mM 0.5150 mL 2.5751 mL 5.1501 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5751 mL 12.8753 mL 25.7506 mL 64.3766 mL
5 mM 0.5150 mL 2.5751 mL 5.1501 mL 12.8753 mL
10 mM 0.2575 mL 1.2875 mL 2.5751 mL 6.4377 mL
15 mM 0.1717 mL 0.8584 mL 1.7167 mL 4.2918 mL
20 mM 0.1288 mL 0.6438 mL 1.2875 mL 3.2188 mL
25 mM 0.1030 mL 0.5150 mL 1.0300 mL 2.5751 mL
30 mM 0.0858 mL 0.4292 mL 0.8584 mL 2.1459 mL
40 mM 0.0644 mL 0.3219 mL 0.6438 mL 1.6094 mL
50 mM 0.0515 mL 0.2575 mL 0.5150 mL 1.2875 mL
60 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0729 mL
80 mM 0.0322 mL 0.1609 mL 0.3219 mL 0.8047 mL
100 mM 0.0258 mL 0.1288 mL 0.2575 mL 0.6438 mL
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CDK8-IN-11 Related Classifications

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-112839338-28-0CDKβ-cateninCyclin dependent kinaseBeta cateninInhibitorinhibitorinhibit

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