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

HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.

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HIF-1α-IN-2 Chemical Structure

HIF-1α-IN-2 Chemical Structure

CAS No. : 2762315-06-8

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Based on 1 publication(s) in Google Scholar

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HIF-1α-IN-2 Related Antibodies

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1 Publications Citing Use of MCE HIF-1α-IN-2

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HIF-1α HIF

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Description

HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation[1].

IC50 & Target

IC50: 28 nM (HIF-1α) in MDA-MB-231, 15 nM (HIF-1α) in MiaPaCa-2[1]
In Vitro

HIF-1α-IN-2 (compound 7f) (5 μM; 72h) suppresses the viability of MDA-MB-231 and MiaPaCa-2 cells with IC50s of 28 nM and 15 nM, respectively[1].
HIF-1α-IN-2 (0-1 μM; 72h) suppresses the expression of HIF-1α and VEGF with dose-dependent effect[1].
HIF-1α-IN-2 (0.25, 0.5, and 1 µM; 16-24h) can significantly inhibit the migration of MDA-MD-231 cells by 56% (0.25 µM), 83% (0.5 µM), and 85% (1 µM), respectively, and also noted in MiaPaCa-2 cells, which demonstrates the unique anti-migration effect of HIF-1α-IN-2[1].
HIF-1α-IN-2 (0-1 μM; 72h) suppresses HIF-1α mRNA levels in MDA-MB-231 cells under hypoxia[1].

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

HIF-1α-IN-2 Related Antibodies

Cell Viability Assay

Cell Line: MDA-MB-231 cells, MiaPaCa-2 cells[1]
Concentration: 5 μM
Incubation Time: 72 hours
Result: Suppressed the viability of these two cell lines with IC50 of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively.

Cell Viability Assay

Cell Line: MDA-MB-231 cells, MiaPaCa-2 cells[1]
Concentration: 5 μM
Incubation Time: 72 hours
Result: Suppressed the viability of these two cell lines with IC50 of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively.
Molecular Weight

361.46

Formula

C21H19N3OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NC(C2=CC(NC3=CC(C)=NC4=CC(OC)=CC=C34)=CC=C2)=CS1
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 : 25 mg/mL (69.16 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 2.7666 mL 13.8328 mL 27.6656 mL
5 mM 0.5533 mL 2.7666 mL 5.5331 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 2.7666 mL 13.8328 mL 27.6656 mL 69.1639 mL
5 mM 0.5533 mL 2.7666 mL 5.5331 mL 13.8328 mL
10 mM 0.2767 mL 1.3833 mL 2.7666 mL 6.9164 mL
15 mM 0.1844 mL 0.9222 mL 1.8444 mL 4.6109 mL
20 mM 0.1383 mL 0.6916 mL 1.3833 mL 3.4582 mL
25 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7666 mL
30 mM 0.0922 mL 0.4611 mL 0.9222 mL 2.3055 mL
40 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7291 mL
50 mM 0.0553 mL 0.2767 mL 0.5533 mL 1.3833 mL
60 mM 0.0461 mL 0.2305 mL 0.4611 mL 1.1527 mL
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HIF-1α-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-1α-IN-22762315-06-8HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHypoxia-inducible factor-1αHIF-1αMigrationAnticancer agentDose-dependentMDA-MB-231MiaPaCa-2 cellsInhibitorinhibitorinhibit

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