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Chemical Structure : SGC-GAK-1
CAS No.: 2226517-76-4
Catalog No.: PC-35852Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 25 mg | $368 | In stock | |
| 100 mg | $958 | In stock | |
| 1 g | Get quote |
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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, 16,000-fold selectivity over NAK; SGC-GAK-1 is highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target; shows high affinity for GAK in cells in cellular target engagement assays (IC50=120 nM), 3-fold selectivity over RIPK2 in cells (IC50=360 nM); robustly blocked growth of 22Rv1 and LNCaP cell lines (Viability IC50=0.17 and 0.65 uM) that express AR splice variants associated with poor clinical prognosis, treatment of 22Rv1 cells with led to PARP cleavage, a marker of cells undergoing apoptosis, and an increase in phosphorylated histone H3 Ser10, as had been observed in with GAK targeting siRNA.
| M.Wt | 389.249 | |
| Formula | C18H17BrN2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine |
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1. Asquith CRM, et al. J Med Chem. 2019 Feb 15. doi: 10.1021/acs.jmedchem.8b01213.
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