CDK8-IN-16
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%[1].
Product Specifications
CAS Number
1860885-61-5
UNSPSC
12352005
Target
CDK; STAT; Wnt
Related Pathways
Cell Cycle/DNA Damage; JAK/STAT Signaling; Stem Cell/Wnt
Field of Research
Cancer
Smiles
O=C(N1CC(C1)OC)C2=NC3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC(N)=C3C=C2
Molecular Formula
C23H22N6O2
Molecular Weight
414.46
References & Citations
[1]Mallinger A, et al., 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. ACS Med Chem Lett. 2016 Mar 28;7 (6) :573-8.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CDK19; CDK8
Available Sizes
Frequently Asked Questions
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