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

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°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

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10 mg$55.00
50 mg$195.00
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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

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°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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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