1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. HIF-1 inhibitor-5

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential.

For research use only. We do not sell to patients.

HIF-1 inhibitor-5 Chemical Structure

HIF-1 inhibitor-5 Chemical Structure

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Description

HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential[1].

IC50 & Target

IC50: 2.38 μM (HIF-1)[1]

In Vitro

HIF-1 inhibitor-5 (Compound 16e; 0-4 μM; 24 h) suppresses A549 cell migration and invasion[1].
HIF-1 inhibitor-5 (0-8 μM; 12 h) blocks VEGF-induced tube formation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

HIF-1 inhibitor-5 (Compound 16e; 1.25-20 μM; s.c.; once) inhibits VEGF-induced angiogenesis in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (Compound 16e) 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.
Molecular Weight

465.58

Formula

C28H35NO5

SMILES

O=C(C1=C(C2=C(OC(C)(C=C2)C)C=C1)O)/C=C/C3=CC(C(C=C3)OC)OCCCN4CCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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HIF-1 inhibitor-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
HIF-1 inhibitor-5
Cat. No.:
HY-149260
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