GAK inhibitor 49 hydrochloride

• CAT Number: I044361
• CAS Number: 2930378-91-7
• Molecular Formula: C20H23ClN2O5
• Molecular Weight: 406.86
• Purity: ≥95%
• Synonyms: 6,7-dimethoxy-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine;hydrochloride
• InChI: InChI=1S/C20H22N2O5.ClH/c1-23-16-10-13-14(6-7-21-15(13)11-17(16)24-2)22-12-8-18(25-3)20(27-5)19(9-12)26-4;/h6-11H,1-5H3,(H,21,22);1H
• InChIKey: LOOMZTXOCDWFDB-UHFFFAOYSA-N
• SMILES: COC1=CC(=CC(=C1OC)OC)NC2=C3C=C(C(=CC3=NC=C2)OC)OC.Cl

GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2[1].
GAK inhibitor 49 (compound 49) hydrochloride shows a weak inhibitory effect on AAK1, BMP2K and STK16, with IC50s of 28, 63 and >100μM, respectively[1].

Reference

[1]. Asquith CRM, et al. Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase. ChemMedChem. 2018;13(1):48-66.
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