2. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR Epigenetics TGF-beta/Smad
  3. CDK GSK-3 PKC
  4. CDK8-IN-12

CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent.

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

CDK8-IN-12 Chemical Structure

CDK8-IN-12 Chemical Structure

CAS No. : 2613307-67-6

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Based on 1 publication(s) in Google Scholar

CDK8-IN-12 Related Antibodies

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Description

CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1].

IC50 & Target[1]

CDK8

14 nM (Ki)

GSK-3α

13 nM (Ki)

GSK-3β

4 nM (Ki)

PKCθ

109 nM (Ki)

In Vitro

CDK8-IN-12 (compound 38) selectively inhibits the proliferation of MV4-11 acute myeloid leukaemia cells with a GI50 of 0.36 μM[1].
CDK8-IN-12 (0.36, 0.72 μM; 2 hours) significantly reduces the phosphorylation of serine 727 on STAT1[1].

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

CDK8-IN-12 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.36, 0.72 μM
Incubation Time: 2 hours
Result: Significantly reduced the phosphorylation of serine 727 on STAT1 at concentrations of their respective 1× GI50 values, but barely affected the level of total STAT1.
In Vivo

CDK8-IN-12 (compound 38; IV; 5 mg/kg for rat and 2 mg/kg for mouse) has a T1/2 of 0.9 hours and 0.34 hours for rat and mouse, respectively[1].
Pharmacokinetic Parameters of CDK8-IN-12 [1].

IV (Rat 5 mg/kg) PO (Rat 20 mg/kg)IV (Mouse 2 mg/kg) PO (Mouse 10 mg/kg)
Tmax (h) 0.04 2.75 0.04 0.42
Cmax (μM) 14.4 2.77 3.44 5.01
AUC0-24 (μM∗h) 9.7 14.6 1.39 2.30
T1/2 (ng/mL) 0.9 2.24 0.34 1.11
CL (L/h∗kg) 1.39 3.78
Vss (L/kg) 1.11 1.99
F (%) 38 33

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

381.86

Formula

C21H20ClN3O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NCCC12CCN(C3=C(C4=CC5=CC=CC=C5O4)C=NC=C3Cl)CC2
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 : 66.67 mg/mL (174.59 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 2.6188 mL 13.0938 mL 26.1876 mL
5 mM 0.5238 mL 2.6188 mL 5.2375 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.6188 mL 13.0938 mL 26.1876 mL 65.4690 mL
5 mM 0.5238 mL 2.6188 mL 5.2375 mL 13.0938 mL
10 mM 0.2619 mL 1.3094 mL 2.6188 mL 6.5469 mL
15 mM 0.1746 mL 0.8729 mL 1.7458 mL 4.3646 mL
20 mM 0.1309 mL 0.6547 mL 1.3094 mL 3.2735 mL
25 mM 0.1048 mL 0.5238 mL 1.0475 mL 2.6188 mL
30 mM 0.0873 mL 0.4365 mL 0.8729 mL 2.1823 mL
40 mM 0.0655 mL 0.3273 mL 0.6547 mL 1.6367 mL
50 mM 0.0524 mL 0.2619 mL 0.5238 mL 1.3094 mL
60 mM 0.0436 mL 0.2182 mL 0.4365 mL 1.0912 mL
80 mM 0.0327 mL 0.1637 mL 0.3273 mL 0.8184 mL
100 mM 0.0262 mL 0.1309 mL 0.2619 mL 0.6547 mL
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CDK8-IN-12 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-122613307-67-6CDKGSK-3PKCCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Protein kinase COrallyGSK-3αGSK-3βPCK-θanti-proliferativeMV4-11 cellanti-cancerInhibitorinhibitorinhibit

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