HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50= 560 nM). HIF-1 inhibitor-4 reduces HIF-1α protein levels without affecting mRNA levels.

Physicochemical Properties

Molecular Formula	C18H19IN2O2
Molecular Weight	422.260136842728
Exact Mass	422.049
CAS #	333357-56-5
PubChem CID	589919
Appearance	White to off-white solid powder
LogP	1.9
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	4
Heavy Atom Count	23
Complexity	371
Defined Atom Stereocenter Count	0
SMILES	C(NC1=CC=C(I)C=C1)(=O)C1=CC=C(CN2CCOCC2)C=C1
InChi Key	ZOFBYPLMJZJZIK-UHFFFAOYSA-N
InChi Code	InChI=1S/C18H19IN2O2/c19-16-5-7-17(8-6-16)20-18(22)15-3-1-14(2-4-15)13-21-9-11-23-12-10-21/h1-8H,9-13H2,(H,20,22)
Chemical Name	N-(4-iodophenyl)-4-(morpholin-4-ylmethyl)benzamide
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	Compound 1, HIF-1 Inhibitor-4, inhibits HIF-1 with an IC50 of 560 nM (measured using U251 cells that express the PLAP reporter gene under the VEGF promoter (VEGF-PLAP)). [1].
References	[1]. Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors. Bioorg Med Chem. 2014 Oct 1;22(19):5513-29.

Solubility Data

Solubility (In Vitro)

DMSO : ~25 mg/mL (~59.21 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.11 mg/mL (2.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 11.1 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. Solubility in Formulation 2: ≥ 1.11 mg/mL (2.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 11.1 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	2.3682 mL	11.8410 mL	23.6821 mL
	5 mM	0.4736 mL	2.3682 mL	4.7364 mL
	10 mM	0.2368 mL	1.1841 mL	2.3682 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.