2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. HIF-1/2α-IN-2

HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).

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HIF-1/2α-IN-2 Chemical Structure

HIF-1/2α-IN-2 Chemical Structure

CAS No. : 862974-22-9

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Based on 1 publication(s) in Google Scholar

HIF-1/2α-IN-2 Related Antibodies

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Description

HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2)[1].

IC50 & Target

Iron Sulfur Cluster Assembly 2 (ISCA2), HIF-1/2α[1]
In Vitro

HIF-1/2α-IN-2 (compound #1) (0-25 μM; 24 h) decreases HIF-2α translation instead of transcription, with a downward trend in VEGFA and POU5F1 (HIF-2α target genes) transcription and insignificant effect on EPAS1 (HIF-2α)[1].
HIF-1/2α-IN-2 (0-100 μM, 24 h) inhibits the production of luciferase driven by the HIF-2α Iron-Responsive Element (IRE) luciferase reporter with an IC50 value of 3.9 μM, to block IRE-dependent translation of HIF-2α[1].
HIF-1/2α-IN-2 (0, 10, 50 μM) protects ISCA2 from Pronase-mediated (4 μg/mL) degradation, and (1.5 μM; 24 h) targets ISCA2 to induce iron and metals accumulation in normoxia 786-0 cells[1].
HIF-1/2α-IN-2 (0-100 μM; 24 h) results ISCA2 inhibition and promotes cell death via ferroptosis[1].

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

HIF-1/2α-IN-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: Normoxia 786-0 cells (20%O2) and hypoxic ACHN cells (or 1%O2 for final 24 h to induce HIF expression)
Concentration: 0, 1, 5, 10, 25 μM
Incubation Time: 24 hours
Result: Decreased the protein level of HIF-2α, FTH1, ISCA2, and increased IRP2 protein level at high concentrations over 10 μM in normoxia 786-0 cells.
Dcreased the HIF-2α and FTH1 levels at 1 μM in hypoxic ACHN cells.

Cell Viability Assay[1]

Cell Line: Normoxia 786-0 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Inhibited 786-0 cells viability by inducing ferroptosis, with an IC50 value of 22.0 μM.
Molecular Weight

342.35

Formula

C16H11FN4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=C2N=C(NC3=NN=C(C4=CC=C(F)C=C4)O3)SC2=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (146.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9210 mL 14.6049 mL 29.2099 mL
5 mM 0.5842 mL 2.9210 mL 5.8420 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (14.60 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9210 mL 14.6049 mL 29.2099 mL 73.0247 mL
5 mM 0.5842 mL 2.9210 mL 5.8420 mL 14.6049 mL
10 mM 0.2921 mL 1.4605 mL 2.9210 mL 7.3025 mL
15 mM 0.1947 mL 0.9737 mL 1.9473 mL 4.8683 mL
20 mM 0.1460 mL 0.7302 mL 1.4605 mL 3.6512 mL
25 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9210 mL
30 mM 0.0974 mL 0.4868 mL 0.9737 mL 2.4342 mL
40 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8256 mL
50 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
60 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2171 mL
80 mM 0.0365 mL 0.1826 mL 0.3651 mL 0.9128 mL
100 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
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HIF-1/2α-IN-2 Related Classifications

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-1/2α-IN-2862974-22-9HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHclear cell renal cell carcinomaccRCClipid peroxidationferroptosisxenograft modelorally activeInhibitorinhibitorinhibit

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