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| | SGC-GAK-1 Basic information |
| Product Name: | SGC-GAK-1 | | Synonyms: | SGC-GAK-1;GAK INHIBITOR 1;6-Bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine;4-Quinolinamine, 6-bromo-N-(3,4,5-trimethoxyphenyl)-;6-Bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine;SGCGAK1,Inhibitor,SGC GAK 1,inhibit | | CAS: | 2226517-76-4 | | MF: | C18H17BrN2O3 | | MW: | 389.24 | | EINECS: | | | Product Categories: | API | | Mol File: | 2226517-76-4.mol |  |
| | SGC-GAK-1 Chemical Properties |
| Boiling point | 484.9±45.0 °C(Predicted) | | density | 1.436±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 10 mg/ml) | | pka | 6.43±0.49(Predicted) | | form | powder | | color | white to beige | | 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. |
| | SGC-GAK-1 Usage And Synthesis |
| Description | 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). | | Uses | SGC GAK 1 is a high affinity cyclin G associated kinase (GAK) inhibitor (Kd = 1.9 nM). Exhibited >30-fold selectivity for GAK versus a panel of other kinases. Inhibits GAK in live cell assays (IC50 = 110 nM). | | Biochem/physiol Actions | SGC-GAK-1 (CA93) is an ATP-competitive cyclin G-associated kinase (GAK) inhibitor (Ki = 3.1 nM by ATP site fluorescent tracer displacement assay; KD = 4.5 nM by ITC) that effectively inhibits Dengue viral entry and packaging in cultures (IC50 = 920 nM) without detectable cytotoxicity. SGC-GAK-1 exhibits much reduced affinity toward only 4 other kinases among a panel of ～400 (KD = 1.9 nM/GAK vs. 110 nM/RIPK2, 190 nM/ADCK3, 520 nM/NLK, 980 nM/AVCR1 by ligand competitive binding assay; IC50 = 110 nM/GAK vs. 360 nM/RIPK2 by cellular target engagement assay). SGC-GAK-1N (CA71) is a structure analog and the recommended negative control (GAK KD = 7.1 μM by ligand competitive binding assay; GAK & RIPK2 IC50 >50 μM by cellular target engagement assay). For characterization details of SGC-GAK-1, please visit the SGC-GAK-1 probe summary on the Structural Genomics Consortium (SGC) website.SGC-GAK-1N is the negative control for the active probe, SGC-GAK-1. SGC-GAK-1N is available from Sigma. To learn more about and purchase SGC-GAK-1N, click here.To learn about other SGC chemical probes, visit sigma.com/sgc | | storage | Store at -20°C | | References | 1) Asquith?et al.?(2019),?SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK); J. Med. Chem.,?62?2830 |
| | SGC-GAK-1 Preparation Products And Raw materials |
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