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.

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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.
SMILES

O=C1NCCC12CCN(C3=C(C4=CC5=CC=CC=C5O4)C=NC=C3Cl)CC2
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-12 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-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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