| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
| Targets |
HIF-1 inhibitor-4 targets hypoxia-inducible factor-1 (HIF-1), a transcription factor that mediates cellular responses to hypoxia. HIF-1 regulates the expression of genes involved in angiogenesis, metabolism, cell survival, and invasion. HIF-1 inhibitor-4 reduces HIF-1α protein levels without affecting its mRNA levels, suggesting it may promote HIF-1α degradation or inhibit its translation.
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| 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].
In vitro, HIF-1 inhibitor-4 inhibits HIF-1 with an IC50 of 560 nM. It reduces HIF-1α protein levels without affecting its mRNA levels. HIF-1 inhibitor-4 inhibits HIF-1 reporter gene activity under the VEGF promoter (VEGF-PLAP). It blocks the transcription of HIF-1 target genes. |
| ln Vivo |
In vivo data for HIF-1 inhibitor-4 is not extensively reported in publicly available sources. As a potent HIF-1 inhibitor, the compound has potential applications in animal models of cancer and ischemic diseases where HIF-1 plays a role. By reducing HIF-1α protein levels and inhibiting HIF-1 transcriptional activity, HIF-1 inhibitor-4 could suppress tumor growth and angiogenesis. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro HIF-1 inhibition assay for HIF-1 inhibitor-4 uses cells transfected with a HIF-1 reporter gene under the VEGF promoter (VEGF-PLAP). Cells are treated with varying concentrations of HIF-1 inhibitor-4 under hypoxic conditions, and reporter gene activity is measured. IC50 values are calculated from dose-response curves. HIF-1α protein levels are measured by Western blotting, and mRNA levels are measured by qPCR.
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| Cell Assay |
Cellular assays for HIF-1 inhibitor-4 are conducted in cancer cell lines. Cells are treated with varying concentrations of HIF-1 inhibitor-4 under normoxic or hypoxic conditions. HIF-1α protein levels are measured by Western blotting. HIF-1 transcriptional activity is assessed using reporter gene assays. Cell proliferation and viability are measured using standard assays. The expression of HIF-1 target genes such as VEGF is measured by qPCR or ELISA.
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| Animal Protocol |
In vivo studies for HIF-1 inhibitor-4 would typically involve xenograft mouse models of cancer. The compound would be administered via intraperitoneal or oral routes. Efficacy would be assessed by measuring tumor growth inhibition and angiogenesis. However, specific published in vivo protocols for HIF-1 inhibitor-4 are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HIF-1 inhibitor-4 is not extensively reported. The compound has a molecular weight of 422.26 g/mol and a molecular formula of C18H19IN2O2. It is soluble in DMSO at 25 mg/mL. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for HIF-1 inhibitor-4 is limited. As a research compound, HIF-1 inhibitor-4 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
HIF-1 inhibitor-4 (CAS 333357-56-5) is a potent HIF-1 inhibitor with an IC50 of 560 nM. It reduces HIF-1α protein levels without affecting its mRNA levels. It has a molecular formula of C18H19IN2O2 and a molecular weight of 422.26 g/mol. HIF-1 inhibitor-4 is a valuable research tool for studying hypoxia signaling and cancer.
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| Molecular Formula |
C18H19IN2O2
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|---|---|
| Molecular Weight |
422.260136842728
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| Exact Mass |
422.049
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| CAS # |
333357-56-5
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| PubChem CID |
589919
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NC1=CC=C(I)C=C1)(=O)C1=CC=C(CN2CCOCC2)C=C1
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| InChi Key |
ZOFBYPLMJZJZIK-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-(4-iodophenyl)-4-(morpholin-4-ylmethyl)benzamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~59.21 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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