Protein kinase inhibitor 1 hydrochloride

• CAT Number: I046291
• CAS Number: 2321337-71-5
• Molecular Formula: C18H18ClN5O3S
• Molecular Weight: 419.89
• Purity: ≥95%
• Synonyms: (5E)-5-[[6-oxo-5-(6-piperazin-1-ylpyridin-3-yl)-1H-pyridin-3-yl]methylidene]-1,3-thiazolidine-2,4-dione;hydrochloride
• InChI: InChI=1S/C18H17N5O3S.ClH/c24-16-13(7-11(9-21-16)8-14-17(25)22-18(26)27-14)12-1-2-15(20-10-12)23-5-3-19-4-6-23;/h1-2,7-10,19H,3-6H2,(H,21,24)(H,22,25,26);1H/b14-8+
• InChIKey: PSLSZGRUEDWPNC-XHIXCECLSA-N
• SMILES: C1CN(CCN1)C2=NC=C(C=C2)C3=CC(=CNC3=O)C=C4C(=O)NC(=O)S4.Cl

Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2. Protein kinase inhibitor 1 (Compound A64) is not an effective Cdk1 inhibitor (IC50 > 10 μM). A64 is moderately selective across a panel of kinases, with Kds 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].

Reference

[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.
 [Content Brief]