HIF-1α-IN-2 is a potent HIF-1α inhibitor (antagonist) with anti-cancer effects, with IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively. HIF-1α-IN-2 inhibits HIF-1α expression by blocking transcription and inhibiting protein translation.

Physicochemical Properties

Molecular Formula	C21H19N3OS
Molecular Weight	361.46
Exact Mass	361.124
CAS #	2762315-06-8
PubChem CID	163196195
Appearance	Off-white to light yellow solid powder
LogP	5.2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	4
Heavy Atom Count	26
Complexity	465
Defined Atom Stereocenter Count	0
SMILES	N1C2C(=CC=C(OC)C=2)C(NC2=CC=CC(C3=CSC(C)=N3)=C2)=CC=1C
InChi Key	ILYYBJSTMKDZND-UHFFFAOYSA-N
InChi Code	InChI=1S/C21H19N3OS/c1-13-9-19(18-8-7-17(25-3)11-20(18)22-13)24-16-6-4-5-15(10-16)21-12-26-14(2)23-21/h4-12H,1-3H3,(H,22,24)
Chemical Name	7-methoxy-2-methyl-N-[3-(2-methyl-1,3-thiazol-4-yl)phenyl]quinolin-4-amine
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 (e.g. under nitrogen), avoid exposure to moisture and light.
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	HIF-1α-IN-2 (compound 7f) reduces MDA-MB-231 and MiaPaCa-2 cell survival at 5 μM and 72 hours, respectively, with IC50 values of 28 nM and 15 nM [1]. With a dose-dependent impact, HIF-1α-IN-2 (0.25, 0.5, and 1 µM; 16–24h) can considerably (0–1 µM; 72h) decrease the expression of HIF-1α and VEGF [1]. inhibited the migration of MDA-MD-231 cells at concentrations of 56%, 0.25 µM, 83%, 0.5 µM, and 85%, 1 µM. It was also detected in MiaPaCa-2 cells. This indicates that HIF-1α- HIF-1α-IN-2 (0-1 μM; 72h) suppresses the levels of HIF-1α mRNA in MDA-MB-231 cells when they are hypoxic [1]. The anti-migration action of IN-2 is distinct [1]. viability test
Cell Assay	Viability assay Cell Types: MDA-MB-231 cells, MiaPaCa-2 cells [1] Tested Concentrations: 5 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the viability of these two cell lines, the IC50 in MDA-MB was 28 nM respectively and 15 nM for -231 and MiaPaCa-2 cells, respectively. Cell viability assay Cell Types: MDA-MB-231 cells, MiaPaCa-2 cells [1] Tested Concentrations: 5 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the viability of these two cell lines, the IC50 in MDA- was 28 nM and 15 nM for MB-231 and MiaPaCa-2 cells respectively.
References	[1]. Synthesis and evaluation of biarylquinoline derivatives as novel HIF-1α inhibitors. Bioorg Chem. 2022;121:105681.

Solubility Data

Solubility (In Vitro)

DMSO : ~25 mg/mL (~69.16 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.92 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.92 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 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	2.7666 mL	13.8328 mL	27.6656 mL
	5 mM	0.5533 mL	2.7666 mL	5.5331 mL
	10 mM	0.2767 mL	1.3833 mL	2.7666 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.