| Description | 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. |
| In vitro | Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC 50 s 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 (IC 50 > 10 μM). A64 is moderately selective across a panel of kinases, with K d s 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 IC 50 s of 19 nM (DYRK1A), 62 nM (DYRK1B), and 74 nM (HIPK2)[1]. |
| Target activity | HIPK2:74 nM (IC50), HIPK2:9.5 nM (Kd), HIPK1:136 nM (IC50) |
| molecular weight | 419.88 |
| Molecular formula | C18H18ClN5O3S |
| CAS | 2321337-71-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Miduturu CV, et al. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinaseinhibitors. Chem Biol. 2011 Jul 29;18(7):868-79. |