Protein kinase inhibitors 1 hydrochloride

(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1, 2-dihydro-[3, 3'-bipyridin]-5-yl)methylene)thiazolidine-2, 4-dione hydrochloride

C18H18ClN5O3S

DMSO : 30 mg/mL (71.45 mM; Need ultrasonic)

Protein Tyrosine Kinase/RTK

Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2. IC50 & Target: IC50: 74 nM (HIPK2), 136 nM (HIPK1)^[1]
Kd: 9.5 nM (HIPK2)^[1] In Vitro: Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2. Protein kinase inhibitors 1 (Compound A64) is not an effective Cdk1 inhibitor (IC₅₀ > 10 uM). A64 is moderately selective across a panel of kinases, with K_ds of 3.7 nM (PIM3), 6.1 nM (CSNK2A2), 6.1 nM (CSNK2A2), 8.8 nM (DYRK1A), 9.5 nM (DAPK1), 31 nM (CSNK2A1), 37 nM (PIM1), 130 nM (DRAK2), 150 nM (CLK2), 190 nM (DRAK1), 220 nM (ULK2), 240 nM (CLK1), 250 nM (DYRK2), and 390 nM (ERK8) and IC₅₀s of 19 nM (DYRK1A), 62 nM (DYRK1B), and 74 nM (HIPK2)^[1].