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Description: High affinity cyclin G associated kinase (GAK) inhibitor
Chemical Name: 6-Bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine
Purity: ≥99% (HPLC)

Biological Activity for SGC GAK 1

SGC GAK 1 is a high affinity cyclin G associated kinase (GAK) inhibitor (Kd = 1.9 nM). Exhibits >30-fold selectivity for GAK over a panel of other kinases. Inhibits GAK in live cell assays (IC50 = 110 nM).

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC GAK 1 probe summary on the SGC website.

Compound Libraries for SGC GAK 1

SGC GAK 1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SGC GAK 1

M. Wt 389.24
Formula C18H17BrN2O3
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 2226517-76-4
PubChem ID 50877865
Smiles BrC1=CC2=C(NC3=CC(OC)=C(OC)C(OC)=C3)C=CN=C2C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SGC GAK 1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.92 100
ethanol 19.46 50

Preparing Stock Solutions for SGC GAK 1

The following data is based on the product molecular weight 389.24. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.57 mL 12.85 mL 25.69 mL
5 mM 0.51 mL 2.57 mL 5.14 mL
10 mM 0.26 mL 1.28 mL 2.57 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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References for SGC GAK 1

References are publications that support the biological activity of the product.

Asquith et al (2019) SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK). J.Med.Chem. 62 2830 PMID: 30768268

Asquith et al (2019) Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK). Bioorg.Med.Chem.Lett. 29 1727 PMID: 31129055

If you know of a relevant reference for SGC GAK 1, please let us know.

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Keywords: SGC GAK 1, SGC GAK 1 supplier, SGCGAK1, cyclin, G, associated, kinases, inhibitors, inhibits, serine/threonine, GAK, Other, Kinases, 6564, Tocris Bioscience

Citations for SGC GAK 1

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