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SGC-GAK-1

  Cat. No.:  DC12565   Featured
Chemical Structure
2226517-76-4
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More than 5000 active chemicals with high quality for research!
Field of application
SGC-GAK-1 (GAK inhibitor 1) is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki of 3.2 nM.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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