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You are here:Home-Chemical Inhibitors & Agonists-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-JH-XVI-178
JH-XVI-178

Chemical Structure : JH-XVI-178

CAS No.: 2648453-53-4

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JH-XVI-178

Catalog No.: PC-28201Not For Human Use, Lab Use Only.

JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 with IC50 of 1/2 nM respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 with IC50 of 1/2 nM respectively.
JH-XVI-178 exhibits limited off-target inhibition of only two additional kinases, STK16 (IC50=107 nM) and FLT3 (D835V), with a KINOMEscan selectivity score of S(10) = 0.01 at 1 uM.
JH-XVI-178 shows potent inhibition of pS727-STAT1 with IC50 of 2 nM following 24 h treatment of Jurkat cells.
JH-XVI-178 shows moderate pharmacokinetic properties following oral dosing in mice.

Physicochemical Properties

M.Wt 435.92
Formula C22H22ClN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

8-(3-chloro-5-(1-methyl-1H-indazol-5-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one

References

1. Hatcher JM, et al. ACS Med Chem Lett. 2021 Oct 22;12(11):1689-1693.

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