Protein Kinase Inhibitors 1 Hydrochloride effectively inhibits HIPK2, demonstrating high potency with IC50 values of 136 nM for HIPK1 and 74 nM for HIPK2, alongside a dissociation constant (Kd) of 9.5 nM for HIPK2.

HIPK1:136 nM (IC50), HIPK2:74 nM (IC50), HIPK2:9.5 nM (Kd)

Protein kinase inhibitors 1 hydrochloride displays strong inhibitory action against HIPK2, with IC50 values of 136 nM and 74 nM for HIPK1 and HIPK2, respectively, and exhibits high affinity for HIPK2, as indicated by a Kd of 9.5 nM. This compound, also known as Compound A64, is ineffective as a Cdk1 inhibitor, with an IC50 exceeding 10 μM. A64 demonstrates moderate selectivity when tested against a range of kinases, showing Kd values ranging from 3.7 nM for PIM3 to 390 nM for ERK8, along with IC50 values of 19 nM for DYRK1A, 62 nM for DYRK1B, and 74 nM for HIPK2.