SGC-GAK-1, Cyclin G Associated Kinase (GAK) inhibitor (TBI4796)

Description

Product Details

Formal Name: 6-Bromo-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine

Molecular Formula: C₁₈H₁₇BrN₂O₃

Formula Weight: 389.25

CAS Number: 2226517-76-4

Purity: >99%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in ethanol (up to 10 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Cyclin G Associated Kinase (GAK) inhibitor

Functions

Very 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. Also displays affinity for RIPK2 (KD = 110 nM) and ADCK3 (KD = 190 nM). Has 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).

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml) or in ethanol (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.