A GAK inhibitor
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SGC-GAK-1

Item No. 33229

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine
CAS Number
2226517-76-4
Molecular Formula
C18H17BrN2O3
Formula Weight
389.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 1 mg/ml
λmax
219, 252 nm
SMILES
BrC1=CC2=C(NC3=CC(OC)=C(C(OC)=C3)OC)C=CN=C2C=C1
InChi Code
InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
InChi Key
AUOSKLDNVNGKRR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $41

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    10 mg

    $72

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    25 mg

    $140

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    50 mg

    $255

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    Product Description

    SGC-GAK-1 is an inhibitor of cyclin G-associated kinase (GAK; Ki = 3.1 nM).1 It is greater than 50-fold selective for GAK over a panel of 400 kinases at 1 µM but does bind to RIPK2 in a bioluminescence resonance energy transfer (BRET) engagement assay (IC50 = 360 nM). SCG-GAK-1 reduces the viability of LNCaP and 22Rv1 prostate cancer cells with IC50 values of 0.65 and 0.17 µM, respectively. It also inhibits dengue virus infection in Huh7 cells (EC50 = 0.08 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Asquith, C.R.M., Berger, B.-T., Wan, J., et al. SGC-GAK-1: A chemical probe for cyclin G associated kinase (GAK). J. Med. Chem. 62(5), 2830-2836 (2019).

    2. Saul, S., Pu, S.-Y., Zuercher, W.J., et al. Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines. Bioorg. Med. Chem. Lett. 30(16), 127284 (2020).