STAT5-IN-1 (also known as STAT5 Inhibitor) is a STAT5 (signal transducer and activator of transcription 5) inhibitor with anticancer activity. It inhibits STAT5 with IC50 of 47 μM for STAT5β isoform. STAT5-IN-1 is a cell permeable non-petide nicotinoyl hydrazone (also Chromone‐Based) which suppresses STAT5 via binding to the SH2 domain. STAT5, a transcription factor, is a member of the STAT family of proteins that is implicated in cell growth and differentiation. STAT5 functions in various biological processes such as homeostasis of hematopoietic stem cells, development of blood cells, growth hormone effects, and differentiation of mammary epithelium. STAT5 has been reported as a therapeutic target for the treatment of human cancers.

Physicochemical Properties

Molecular Formula	C16H11N3O3
Molecular Weight	293.28
Exact Mass	293.08
CAS #	285986-31-4
Related CAS #	285986-31-4
PubChem CID	9566174
Appearance	White to light yellow solid powder
Density	1.3±0.1 g/cm3
Index of Refraction	1.657
LogP	1.76
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	3
Heavy Atom Count	22
Complexity	501
Defined Atom Stereocenter Count	0
SMILES	C1=CC=C2C(=C1)C(=O)C(=CO2)/C=N/NC(=O)C3=CN=CC=C3
InChi Key	DAVIKTBRCQWOGT-GIJQJNRQSA-N
InChi Code	InChI=1S/C16H11N3O3/c20-15-12(10-22-14-6-2-1-5-13(14)15)9-18-19-16(21)11-4-3-7-17-8-11/h1-10H,(H,19,21)/b18-9+
Chemical Name	N′-((4-Oxo-4H-chromen-3-yl)methylene)nicotinohydrazide
Synonyms	STAT5 Inhibitor; STAT5-Inhibitor;STAT5-IN-1
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

ln Vitro	A member of the STAT protein family, signal transducer and activator of transcription 5 (STAT5) is connected to the development and maturation of cells. By attaching itself to the SH2 domain, STAT5-IN-1 suppresses STAT5. There is a slight inhibition of the tyrosine kinase Lck's and STAT3, STAT1, and SH2 domain functions (IC50>500 μM). In K562 nuclear extracts, STAT5-IN-1 inhibits the binding of STAT5 and STAT5 DNA. The activity of STAT5-IN-1 against STAT5β is unaffected by the substitution of an ethyl group for the hydrogen at position C6 in the chromone ring, but all selectivity against other STAT family members is lost[1].
ln Vivo
Animal Protocol
References	[1]. Discovery of chromone-based inhibitors of the transcription factor STAT5. Chembiochem. 2008 Mar 25;9(5):723-7.
Additional Infomation	N'-[(4-oxo-4H-chromen-3-yl)methylene]nicotinohydrazide is a carbohydrazide that is nicotinohydrazide in which the terminal nitrogen has undergone formal condensation with the aldehyde group of 4-oxo-4H-chromene-3-carbaldehyde. It is an inhibitor of STAT5 (Signal Transducer and Activator of Transcription 5) protein. It has a role as a signal transducer and activator of transcription 5 protein inhibitor. It is a carbohydrazide, a member of chromones and a member of pyridines.

Solubility Data

Solubility (In Vitro)

DMSO:≥ 20 mg/mL Water:<1mg/mL Ethanol:<1mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2 mg/mL (6.82 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 20.0 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	3.4097 mL	17.0486 mL	34.0971 mL
	5 mM	0.6819 mL	3.4097 mL	6.8194 mL
	10 mM	0.3410 mL	1.7049 mL	3.4097 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.