HIF-1 inhibitor-5

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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

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Purity & Documentation
References
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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 administration^a^[1]

Parameter	iv (20 mg/kg) (n = 2)
T_max (h)	0.033
C_max (μmol/L)	7.06
T_1/2 (h)	1.64
CL (mL/h)	2368.50
V_Z (L)	5.59
AUC_0-t (μmol•h/L)	5.27
AUC_0-∞ (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

Handling Instructions (2659 KB)

References

[1]. Xu H, et al. Design, synthesis and evaluation of the novel chalcone derivatives with 2,2-dimethylbenzopyran as HIF-1 inhibitors that possess anti-angiogenic potential. Eur J Med Chem. 2023 Mar 15;250:115171. [Content Brief]

HIF-1 inhibitor-5 Related Classifications

Cardiovascular Disease

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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.

Keywords:

HIF-1 inhibitor-5HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHanti-angiogenicA549VEGFHUVECInhibitorinhibitorinhibit

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