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SGC-GAK-1 | Potent and selective Cyclin G Associated Kinase (GAK) inhibitor

SGC-GAK-1 (2226517-76-4) is a highly potent and selective inhibitor of cyclin G associated kinase (GAK), a member of the numb-associated kinase (NAK) family involved in membrane trafficking and sorting of proteins and is required for the maintenance of centrosome maturation and progression though mitosis. KD = 1.9 nM with >50-fold selectivity against a panel of 400 kinases. It also displayed affinity for RIPK2 (KD = 110 nM) and ADCK3 (KD = 190 nM). SGC-GAK-1 displayed potent cellular activity in HEK293T cells (IC50 = 120 nM) and showed strong growth inhibition in the prostate cancer cell lines LNCaP (IC50 = 0.65 µM) and 22Rv1 (IC50 = 0.17 µM).

References/Citations
1) Asquith et al. (2019), SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK); J. Med. Chem., 62 2830

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Catalog#  10-4796-0010

$55.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
2226517-76-4
Catalog Number:
10-4796
Activity:
Potent and selective Cyclin G Associated Kinase (GAK) inhibitor
Chemical Name:
6-Bromo-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine
Molecular Weight:
389.25
Molecular Formula:
C18H17BrN2O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 10 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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