IL-4-inhibitor-1 (compound 52) is an inhibitor (blocker/antagonist) of IL-4 with EC50 of 1.81 µM.

Physicochemical Properties

Molecular Formula	C18H12FN3O2
Molecular Weight	321.31
Exact Mass	321.091
CAS #	1332184-63-0
PubChem CID	136164931
Appearance	Light yellow to yellow solid powder
Density	1.5±0.1 g/cm3
Boiling Point	590.6±50.0 °C at 760 mmHg
Flash Point	311.0±30.1 °C
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.729
LogP	3.17
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	2
Heavy Atom Count	24
Complexity	474
Defined Atom Stereocenter Count	0
InChi Key	DWZPPBGRCDPFSS-UHFFFAOYSA-N
InChi Code	InChI=1S/C18H12FN3O2/c19-12-4-1-10(2-5-12)15-8-13(14(9-20)18(21)22-15)11-3-6-16(23)17(24)7-11/h1-8,23-24H,(H2,21,22)
Chemical Name	2-amino-4-(3,4-dihydroxyphenyl)-6-(4-fluorophenyl)pyridine-3-carbonitrile
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
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

Targets	EC50: 1.81 µM (IL-4)[1].
ln Vitro	Compound 52, known as IL-4-inhibitor-1, showed functional disruption of type II IL-4 binding in a cellular environment with low micromolar affinity[1]. Compound 52, also known as IL-4-inhibitor-1, demonstrates a dose-dependent decrease in pSTAT-6 levels, with an EC50 value of 3.1 µM. However, it had no effect on STAT-6 levels[1].
References	[1]. A Small-Molecule Inhibitor to the Cytokine Interleukin-4. ACS Chem Biol. 2020 Oct 16;15(10):2649-2654.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (311.23 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (7.78 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.1123 mL	15.5613 mL	31.1226 mL
	5 mM	0.6225 mL	3.1123 mL	6.2245 mL
	10 mM	0.3112 mL	1.5561 mL	3.1123 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.