GAK inhibitor 49 hydrochloride is an ATP-competitive, novel cyclin G-associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cellular IC50 of 56 nM. It has also been demonstrated that GAK inhibitor 49 hydrochloride binds to RIPK2.

Physicochemical Properties

Molecular Formula	C20H23CLN2O5
Molecular Weight	406.86
CAS #	2930378-91-7
Appearance	White to yellow solid powder
Synonyms	GAK inhibitor 49 hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	GAK inhibitor 49 (compound 49) hydrochloride has IC50 values of 28, 63, and >100μM, respectively, indicating a modest inhibitory impact on AAK1, BMP2K, and STK16[1].
References	[1]. Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase. ChemMedChem. 2018;13(1):48-66.

Solubility Data

Solubility (In Vitro)

DMSO : ~14.29 mg/mL (~35.1 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.43 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4578 mL	12.2892 mL	24.5785 mL
	5 mM	0.4916 mL	2.4578 mL	4.9157 mL
	10 mM	0.2458 mL	1.2289 mL	2.4578 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.