SGC-GAK-1 | GAK inhibitor | Probechem Biochemicals

Chemical Structure : SGC-GAK-1

CAS No.: 2226517-76-4

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SGC-GAK-1 (GAK inhibitor 1)

货号: 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, 16,000-fold selectivity over NAK.

规格	价格	库存
5 mg	￥880	In stock
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.
SGC-GAK-1 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).
SGC-GAK-1 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.

物理化学性质&存储条件

分子量	389.249
分子式	C18H17BrN2O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine

参考文献

1. Asquith CRM, et al. J Med Chem. 2019 Feb 15. doi: 10.1021/acs.jmedchem.8b01213.

SGC-GAK-1 (GAK inhibitor 1)

生物&药学活性

物理化学性质&存储条件

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SGC-GAK-1 (GAK inhibitor 1)

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物理化学性质&存储条件

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