HIF-2α-IN-4 is a potent HIF-2α translation inhibitor (antagonist) with IC50 of 5 μM. HIF-2α-IN-4 reduces constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links the 5'UTR iron-responsive element to oxygen sensing.

Physicochemical Properties

Molecular Formula	C9H9N3O4S2
Molecular Weight	287.315459012985
Exact Mass	287.003
CAS #	882268-69-1
PubChem CID	2820256
Appearance	Light yellow to yellow solid powder
LogP	2.1
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Heavy Atom Count	18
Complexity	500
Defined Atom Stereocenter Count	0
SMILES	N#CC(S(C)(=O)=O)=NNC1=C(C(OC)=O)SC=C1
InChi Key	OOGAPDPPVHJYGJ-UHFFFAOYSA-N
InChi Code	InChI=1S/C9H9N3O4S2/c1-16-9(13)8-6(3-4-17-8)11-12-7(5-10)18(2,14)15/h3-4,11H,1-2H3
Chemical Name	methyl 3-[2-[cyano(methylsulfonyl)methylidene]hydrazinyl]thiophene-2-carboxylate
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: This product requires protection from light (avoid light exposure) during transportation and storage.
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	In a mTOR-independent way, HIF-2α-IN-4 (Compound 76) (10 μM; 786-O cells) decreases the translation of HIF-2α mRNA [1]. In both normal and hypoxic oxygen circumstances, HIF-2α-IN-4 decreases the expression of HIF-2α target genes and HIF-2α protein [1].
References	[1]. Small-molecule inhibitors of HIF-2α translation link its 5'UTR iron-responsive element to oxygen sensing. Mol Cell. 2008;32(6):838-848.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~174.02 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (8.70 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	3.4804 mL	17.4022 mL	34.8044 mL
	5 mM	0.6961 mL	3.4804 mL	6.9609 mL
	10 mM	0.3480 mL	1.7402 mL	3.4804 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.