CDK8-IN-16 (Compound 51) is an orally active dual inhibitor of CDK8 and CDK19 with IC50 of 5.1 nM and 5.6 nM, respectively. CDK8-IN-16 inhibits STAT1SER727 phosphorylation in SW620 cells with IC50 of 17.9 nM and inhibits WNT signaling in 7dF3 cells with IC50 of 7.2 nM. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.

Physicochemical Properties

Molecular Formula	C23H22N6O2
Molecular Weight	414.46
CAS #	1860885-61-5
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	CDK8 5.1 nM (IC50); CDK19 5.6 nM (IC50)
References	[1]. 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.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4128 mL	12.0639 mL	24.1278 mL
	5 mM	0.4826 mL	2.4128 mL	4.8256 mL
	10 mM	0.2413 mL	1.2064 mL	2.4128 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.