ML228
Based on 7 publication(s) in Google Scholar
ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 1357171-62-0
- Fòrmula: C27H21N5
- Peso molecular:415.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ML228
More- Mol Cancer. 2022 Jun 23;21(1):135. [Abstract]
- Biochem Pharmacol. 2024 May 14:225:116294. [Abstract]
- Int J Mol Sci. 2024 Jan 24;25(3):1442. [Abstract]
- Oncol Rep. 2020 Jul;44(1):103-114. [Abstract]
- J Chem Neuroanat. 2021 Oct:116:101994. [Abstract]
- Biochem Biophys Res Commun. 2023 Jun 30:663:192-201. [Abstract]
- Exp Ther Med. 2017 Mar;13(3):861-866. [Abstract]
Actividad biológica
EC50: 1 μM (HIF)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | EC50 |
1.12 μM
Compound: ML228
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Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
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[PMID: 22172704] |
| U2OS | EC50 |
1.4 μM
Compound: ML228
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Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
Activation of GFP-tagged HIF1alpha expressed in human U2OS cells assessed as HIF1alpha nuclear translocation by high content imaging assay
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[PMID: 22172704] |
| U2OS | EC50 |
1.63 μM
Compound: ML228
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Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
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[PMID: 22172704] |
| U2OS | EC50 |
15.6 μM
Compound: ML228
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Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM iron
Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM iron
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[PMID: 22172704] |
| U2OS | EC50 |
5.01 μM
Compound: ML228
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Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM zinc
Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay in presence of 50 uM zinc
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[PMID: 22172704] |
ML228 (CID-46742353) represents a novel chemotype available to the research community for the study of HIF activation and its therapeutic potential. Not only is the compound substantially different in structure from known HIF activators, ML228 lacks the acidic functional group almost universally present in PHD inhibitors, which may be important for certain disease applications[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rat[3]
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Dosage:1 µg/kg
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Administration:injection; 7 days
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Result:Alleviated SCI of the central nervous system and relieve associated symptoms.
Chemical Information
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No. CAS 1357171-62-0
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Appearance Solid
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Peso molecular 415.49
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Fòrmula C27H21N5
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Color Light yellow to yellow
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SMILES
C1(C2=NC=CC=C2)=NC(NCC3=CC=C(C4=CC=CC=C4)C=C3)=C(C5=CC=CC=C5)N=N1
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Synonyms
CID-46742353
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Mol Cancer
circEXOC6B interacting with RRAGB, an mTORC1 activator, inhibits the progression of colorectal cancer by antagonizing the HIF1A-RRAGB-mTORC1 positive feedback loop. [Abstract]2022 Jun 23;21(1):135. PMID: 35739524 -
Biochem Pharmacol
Dihydroartemisinin breaks the positive feedback loop of YAP1 and GLUT1-mediated aerobic glycolysis to boost the CD8+ effector T cells in hepatocellular carcinoma. [Abstract]2024 May 14:225:116294. PMID: 38754557 -
Int J Mol Sci
The HIF-1α/EGF/EGFR Signaling Pathway Facilitates the Proliferation of Yak Alveolar Type II Epithelial Cells in Hypoxic Conditions. [Abstract]2024 Jan 24;25(3):1442. PMID: 38338723 -
Oncol Rep
Knockdown of KRT17 decreases osteosarcoma cell proliferation and the Warburg effect via the AKT/mTOR/HIF1α pathway. [Abstract]2020 Jul;44(1):103-114. PMID: 32627037 -
J Chem Neuroanat
HIF-1α aggravated traumatic brain injury by NLRP3 inflammasome-mediated pyroptosis and activation of microglia. [Abstract]2021 Oct:116:101994. PMID: 34166779 -
Biochem Biophys Res Commun
Hydrogen inhalation therapy regulates lactic acid metabolism following subarachnoid hemorrhage through the HIF-1α pathway. [Abstract]2023 Jun 30:663:192-201. PMID: 37141668 -
Exp Ther Med
Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats. [Abstract]2017 Mar;13(3):861-866. PMID: 28450910
Solvente y solubilidad
DMSO : ≥ 35 mg/mL (84.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Theriault JR, et al. Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway. Probe Reports from the NIH Molecular Libraries Program. [Content Brief]
[2]. Theriault JR, et al. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. [Content Brief]
[3]. Chen H, et al. Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats.Exp Ther Med. 2017 Mar;13(3):861-866. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4068 mL | 12.0340 mL | 24.0680 mL | 60.1699 mL |
| 5 mM | 0.4814 mL | 2.4068 mL | 4.8136 mL | 12.0340 mL | |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4068 mL | 6.0170 mL | |
| 15 mM | 0.1605 mL | 0.8023 mL | 1.6045 mL | 4.0113 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2034 mL | 3.0085 mL | |
| 25 mM | 0.0963 mL | 0.4814 mL | 0.9627 mL | 2.4068 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8023 mL | 2.0057 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5042 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 1.2034 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL |
ML228 Related Classifications
HY-12754 Related Classifications
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