2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. GN44028

GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.

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

GN44028 Chemical Structure

GN44028 Chemical Structure

CAS No. : 1421448-26-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
1 mg USD 133 In-stock
5 mg USD 280 In-stock
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Based on 4 publication(s) in Google Scholar

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HIF-1α HIF

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  • Purity & Documentation

  • References

  • Customer Review

Description

GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers[1][3].

IC50 & Target

IC50: 14 nM (HIF-1α)[1].
In Vitro

GN44028 (compound 2I, 0-30 µM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells[1].
GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells[1].
GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells[2].

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

GN44028 Related Antibodies

RT-PCR[1]

Cell Line: HeLa cells
Concentration: 0.001, 0.01, 0.1, 1µM
Incubation Time: 4 h
Result: Inhibited the hypoxia-induced HIF-1 transcriptional activity without affecting HIF-1α/HIF-1β heterodimerization.
In Vivo

GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells[3].
GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model[2].

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

Animal Model: Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells[3]
Dosage: 10 mg/kg
Administration: Oral gavage
Result: Reduced both proneural and mesenchymal markers.
Animal Model: Subcutaneous colorectal cancer model (HCT116)[2]
Dosage: 5 mg/kg
Administration: Tail vein injection, twice a week
Result: Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.
Molecular Weight

305.33

Formula

C18H15N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(NC2=CC=C(OCCO3)C3=C2)=NNC4=C1CC5=CC=CC=C45
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (163.76 mM; Need ultrasonic; 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 3.2751 mL 16.3757 mL 32.7515 mL
5 mM 0.6550 mL 3.2751 mL 6.5503 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. 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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 (8.19 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 (8.19 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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).
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

Purity: 99.48%

COA (245 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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. 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 3.2751 mL 16.3757 mL 32.7515 mL 81.8786 mL
5 mM 0.6550 mL 3.2751 mL 6.5503 mL 16.3757 mL
10 mM 0.3275 mL 1.6376 mL 3.2751 mL 8.1879 mL
15 mM 0.2183 mL 1.0917 mL 2.1834 mL 5.4586 mL
20 mM 0.1638 mL 0.8188 mL 1.6376 mL 4.0939 mL
25 mM 0.1310 mL 0.6550 mL 1.3101 mL 3.2751 mL
30 mM 0.1092 mL 0.5459 mL 1.0917 mL 2.7293 mL
40 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0470 mL
50 mM 0.0655 mL 0.3275 mL 0.6550 mL 1.6376 mL
60 mM 0.0546 mL 0.2729 mL 0.5459 mL 1.3646 mL
80 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0235 mL
100 mM 0.0328 mL 0.1638 mL 0.3275 mL 0.8188 mL
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GN44028 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:

GN440281421448-26-1GN 44028GN-44028HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHypoxiaHeLaheterodimerizationHCT116colorectal cancerGSCsPN12ME23cancerInhibitorinhibitorinhibit

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