SGC-GAK-1|GAK inhibitor 1

Cas No.:	2226517-76-4
Chemical Name:	6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
Synonyms:	GAK inhibitor 1
SMILES:	N1C2C(=CC(Br)=CC=2)C(NC2=CC(OC)=C(OC)C(OC)=C2)=CC=1
Formula:	C₁₈H₁₇BrN₂O₃
M.Wt:	389.249
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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].
Target:	Ki: 3.1 nM (GAK)[1]
In Vitro:	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]. Cell Viability Assay[1] Cell Line: Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145) Concentration: 0.1, 1, and 10 µM Incubation Time: 48 hours or 72 hours Result: Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50s of 0.05±0.15 µM and 0.17±0.65 µM, respectively.
References:	[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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