SGC-GAK-1 | Potent and selective Cyclin G Associated Kinase (GAK) inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 10 mg | $55.00 | ||
| 50 mg | $195.00 |
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
NMR (Conforms)
Safety Data Sheet:
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
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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