SGC-GAK-1
Synonym(s):6-Bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine;CA93
- CAS NO.:2226517-76-4
- Empirical Formula: C18H17BrN2O3
- Molecular Weight: 389.24
- MDL number: MFCD31689258
- Update Date: 2023-06-30 15:45:59
What is SGC-GAK-1?
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).
The Uses of SGC-GAK-1
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
Properties of SGC-GAK-1
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. |
Safety information for SGC-GAK-1
Computed Descriptors for SGC-GAK-1
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Ivermectin EP Impurity B Fosfomycin EP impurity D Rimegepant Impurity 3 Tubulysin D Tubulysin F Tubulysin A Tubulysin E Potassium HMDS (1.0 M in THF) 4-chloro-5-nitropyridin-2-amine 5-bromo-6-methyl-3-nitropyridin-2-amine 4-bromo-6-chloropicolinic acid 5-bromo-4-chloropyridin-2-amine 2-bromo-5-methylpyridin-4-amine 5-bromo-2-chloroisonicotinic acid (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Imeglimin Hydrochloride IH 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Fuel shell 1-(4-Aminophenyl)-3-morpholino-5,6-dihydropyridin-2(1H)-one Methyl 4-amino-3-(piperidin-1-yl)benzoateRelated products of tetrahydrofuran
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