SGC-GAK-1

• CAT Number: I014677
• CAS Number: 2226517-76-4
• Molecular Formula: C18H17BrN2O3
• Molecular Weight: 389.24
• Purity: ≥95%
• Synonyms: 6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
• InChI: InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
• InChIKey: AUOSKLDNVNGKRR-UHFFFAOYSA-N
• SMILES: COC1=CC(=CC(=C1OC)OC)NC2=C3C=C(C=CC3=NC=C2)Br

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK[1].
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with Kis of 3.1 nM, 53 μM, 51 μM, respectively[1].
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with KDs of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively[1].
SGCGAK-1 (0.1, 1, and 10 μM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 μM, but minimal effect in PC3 and DU145 cells[1].

Reference

[1]. Asquith CRM, et al. SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). J Med Chem. 2019 Feb 26.
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