| Field | Specification |
|---|---|
| Applications | |
| Molecular weight | |
| Molecular formula | C28H35NO5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
HIF-1 inhibitor-5 is a potent inhibitor of HIF-1, with an IC50 of 2.38 μM, and it possesses anti-angiogenic potential[1]. It has the molecular formula C28H35NO5 and a molecular weight of 465.58 g/mol.
Physical & Chemical Properties
| Molecular Formula | C28H35NO5 |
|---|---|
| Molecular Weight | 465.58 g/mol |
| SMILES | O=C(C1=C(C2=C(OC(C)(C=C2)C)C=C1)O)/C=C/C3=CC(C(C=C3)OC)OCCCN4CCCC4 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 2.38 μM (HIF-1)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Migration and invasion of A549 cells are suppressed by HIF-1 inhibitor-5 (0-4 μM; 24 h)[1]. Tube formation induced by VEGF is blocked by HIF-1 inhibitor-5 (0-8 μM; 12 h)[1].
Cell Cytotoxicity Assay[1]
| Cell Line | A549 and HUVEC cells |
|---|---|
| Concentration | 0-128 μM |
| Incubation Time | 48 h |
| Result | Showed cytotoxic effects with IC50s of 8.883 μM and 19.599 μM for A549 and HUVEC cells, respectively. |
Cell Migration Assay [1]
| Cell Line | A549 cell |
|---|---|
| Concentration | 0, 2 and 4 μM |
| Incubation Time | 24 h |
| Result | The number of migrated A549 cells decreased significantly. |
Cell Invasion Assay[1]
| Cell Line | A549 cell |
|---|---|
| Concentration | 0, 2 and 4 μM |
| Incubation Time | 24 h |
| Result | Inhibited cell invasion at a concentration-dependent manner. |
In Vivo
In mice, HIF-1 inhibitor-5 (1.25-20 μM; s.c.; once) inhibits VEGF-induced angiogenesis[1].
| Animal Model | C57/bl6 female mice, VEGF-induced angiogenesis model[1] |
|---|---|
| Dosage | 1.25, 5 and 20 μM |
| Administration | 0.5 mL of matrix glue subcutaneously injected near the midline of abdomen |
| Result | Decreased the number of blood vessels. |
| Animal Model | SD rats |
|---|---|
| Dosage | 20 mg/kg |
| Administration | Intravenous administration (Pharmacokinetic Study) |
| Result | Pharmacokinetic parameters of HIF-1 inhibitor-5 in rats after intravenous administrationa[1] Parameter iv (20 mg/kg) (n = 2) Tmax (h) 0.033 Cmax (μmol/L) 7.06 T1/2 (h) 1.64 CL (mL/h) 2368.50 VZ (L) 5.59 AUC0-t (μmol•h/L) 5.27 AUC0-∞ (μmol•h/L) 8.88 aAfter administration, blood samples were collected at different time (0, 0.083, 0.17, 0.5, 1, 2, 4, 6 h). The combination of compounds in a ratio of 8% ethanol absolute, 4% Tween-80 and 88% normal saline was chosen for the intravenous injection formulation. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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