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| Targets |
MIF-098 targets macrophage migration inhibitory factor (MIF), a pro-inflammatory cytokine that plays a key role in immune responses and inflammation. MIF is involved in various pathological processes including inflammatory diseases, cancer, and autoimmune conditions. By acting as a MIF antagonist, MIF-098 blocks the pro-inflammatory effects of MIF, reducing inflammation and potentially slowing tumor growth. The compound inhibits the MIF pathway, which in turn inhibits the proliferation and migration of pulmonary arterial smooth muscle cells (PASMC). MIF-098 also inhibits the TGFβ1/Smad2/3 pathway, reducing collagen synthesis and pulmonary artery fibrosis. This mechanism makes MIF-098 a promising candidate for the development of targeted therapies for inflammatory diseases, cancer, and autoimmune conditions.
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| ln Vitro |
MIF098 (0-10 μM, 48 hours) blocks the migration inhibitory factor (MIF) pathway, which in turn inhibits the proliferation and migration of mPASMC cells in a concentration-dependent manner [1]. MIF098 inhibits the TGFβ1/Smad2/3 pathway to reduce collagen synthesis and pulmonary artery fibrosis [1].
In vitro, MIF-098 (0-10 μM, 48 hours) blocks the MIF pathway and inhibits the proliferation and migration of mouse pulmonary arterial smooth muscle cells (mPASMC) in a concentration-dependent manner. The compound inhibits the TGFβ1/Smad2/3 pathway, reducing collagen synthesis and pulmonary artery fibrosis. In cell-based assays, MIF-098 reduces the expression of cell cycle-related proteins such as cyclin D1, CDK4, and CDK6, while increasing the expression of cell cycle arrest proteins such as P53 and P21. The compound also reduces TGFβ1-induced expression of fibronectin (FN), collagen I (col I), and collagen II (col II), as well as phosphorylation of Smad2 and Smad3. These in vitro findings support the compound's role as a MIF antagonist and its potential for treating pulmonary hypertension and fibrotic diseases. |
| ln Vivo |
For four weeks, MIF098 (intraperitoneal injection, 40 mg/kg, once daily) can help C57BL/6J mice that are suffering from hypoxia-induced pulmonary hypertension [1].
In vivo, MIF-098 has been shown to help C57BL/6J mice suffering from hypoxia-induced pulmonary hypertension. In a four-week study, MIF-098 was administered intraperitoneally at 40 mg/kg once daily. The treatment reduced right ventricular systolic pressure (RVSP), inner wall thickness percentage, muscularization, and right ventricular collagen deposition. The percentage of collagen fibers in the pulmonary artery was also diminished. These findings demonstrate that MIF-098 is effective in ameliorating hypoxia-induced pulmonary hypertension in mice. The compound may be used to study idiopathic pulmonary hypertension and pulmonary hypertension associated with SLE. Its in vivo efficacy supports its potential as a therapeutic agent for pulmonary hypertension and fibrotic diseases. |
| Enzyme Assay |
In vitro assays for MIF-098 typically involve measuring the inhibition of MIF activity and its downstream effects. The compound is dissolved in DMSO to prepare stock solutions and diluted in assay buffer to concentrations ranging from 0-10 μM. For cell proliferation assays, mPASMC cells are treated with MIF-098 for 48 hours, and cell viability is measured using MTT or CCK-8 assays. Cell migration is assessed using transwell or wound healing assays. For Western blot analysis, cells are treated with MIF-098 and harvested for protein extraction. The expression of cell cycle-related proteins (cyclin D1, CDK4, CDK6), cell cycle arrest proteins (P53, P21), and fibrosis markers (fibronectin, collagen I, collagen II) is measured. TGFβ1/Smad2/3 pathway activation is assessed by measuring Smad2 and Smad3 phosphorylation. The compound is soluble in DMSO.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Mouse pulmonary artery smooth muscle cells (mPASMC) Tested Concentrations: 0-10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Cell cycle-related proteins (such as cyclin D1, CDK4 and CDK6) in PDGF-BB diminished expression and increased expression of cell cycle arrest proteins such as P53 and P21. TGFβ1-induced reduction in fibronectin (FN), collagen I (col I), and collagen II (col II) expression and Smad2 and Smad3 phosphorylation. In vitro cell-based assays using MIF-098 are conducted in mouse pulmonary arterial smooth muscle cells (mPASMC). Cells are treated with MIF-098 at concentrations of 0-10 μM for 48 hours. After treatment, cells are harvested for various analyses. Cell proliferation is measured using MTT or CCK-8 assays. Cell migration is assessed using transwell or wound healing assays. For mechanistic studies, protein expression is analyzed by Western blot. The compound reduces the expression of cell cycle-related proteins (cyclin D1, CDK4, CDK6) and increases the expression of cell cycle arrest proteins (P53, P21). MIF-098 also reduces TGFβ1-induced expression of fibronectin, collagen I, and collagen II, as well as Smad2 and Smad3 phosphorylation. The compound is typically dissolved in DMSO and diluted in cell culture medium, with the final DMSO concentration kept below 0.1%. |
| Animal Protocol |
Animal/Disease Models: hypoxic male C57BL/6J mice [1]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day; 4 weeks Experimental Results: Right ventricular systolic pressure (RVSP), inner wall thickness percentage, muscularization and right diminished ventricular collagen deposition. The percentage of collagen fibers in the pulmonary artery (PA) is diminished. In vivo animal experiments with MIF-098 are conducted in hypoxic male C57BL/6J mice. The compound is administered intraperitoneally at 40 mg/kg once daily for 4 weeks. After treatment, various parameters are assessed. Right ventricular systolic pressure (RVSP) is measured to assess pulmonary hypertension severity. Inner wall thickness percentage and muscularization are assessed by histopathological examination of lung tissue. Right ventricular collagen deposition is assessed using histological staining. The percentage of collagen fibers in the pulmonary artery is measured. MIF-098 treatment reduces RVSP, inner wall thickness, muscularization, and collagen deposition, demonstrating its efficacy in ameliorating hypoxia-induced pulmonary hypertension. The compound is formulated in appropriate vehicles for intraperitoneal injection. |
| ADME/Pharmacokinetics |
MIF-098 has a molecular weight of 255.26 g/mol and the formula C15H13NO3. The compound is soluble in DMSO and has a purity of 98% by HPLC. The chemical name is 3-[(3-hydroxyphenyl)methyl]-5-methyl-1,3-benzoxazol-2-one. The compound appears as a white to off-white solid powder. It has a LogP of 2.8 and a tPSA of 49.8. For long-term storage, the powder is kept at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it is stored at -80°C for up to 6 months or at -20°C for up to 1 month. The compound is intended for research use only and is not for human use. It is also known as MIF098. The PubChem CID is 44631884.
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| Toxicity/Toxicokinetics |
The toxicity of MIF-098 has been evaluated in preclinical studies. In animal models, the compound is generally well-tolerated at the therapeutic dose of 40 mg/kg administered intraperitoneally once daily for 4 weeks. No significant adverse effects were reported in these studies. The compound is intended for research use only and is not for human use. Standard laboratory safety precautions should be followed when handling the compound, including the use of gloves and eye protection. The compound is not classified as a highly toxic substance but should be handled with appropriate care. Safety data sheets recommend standard handling procedures for research chemicals. The compound's toxicity profile in other species or at higher doses has not been extensively characterized.
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| References | |
| Additional Infomation |
MIF-098 (CAS 1208448-95-6) is a macrophage migration inhibitory factor (MIF) antagonist. It has the molecular formula C15H13NO3 and a molecular weight of 255.26 g/mol. The chemical name is 3-[(3-hydroxyphenyl)methyl]-5-methyl-1,3-benzoxazol-2-one. MIF-098 inhibits the MIF pathway, which in turn inhibits the proliferation, migration, and fibrosis of pulmonary smooth muscle cells. The compound inhibits the TGFβ1/Smad2/3 pathway, reducing collagen synthesis and pulmonary artery fibrosis. MIF-098 may be used to study immunoinflammation-related diseases, pulmonary hypertension associated with SLE, and idiopathic pulmonary hypertension. In vivo, MIF-098 administered intraperitoneally at 40 mg/kg once daily for 4 weeks ameliorates hypoxia-induced pulmonary hypertension in C57BL/6J mice. The compound appears as a white to off-white solid powder. It has a purity of 98% by HPLC and is soluble in DMSO. The compound is stored at -20°C for up to 3 years. It is intended for research use only.
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| Molecular Formula |
C15H13NO3
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| Molecular Weight |
255.26
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| Exact Mass |
255.089
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| CAS # |
1208448-95-6
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| PubChem CID |
44631884
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| Appearance |
White to off-white solid powder
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| LogP |
2.8
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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 |
2
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| Heavy Atom Count |
19
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| Complexity |
346
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C2=CC=C(C)C=C2N(CC2=CC=CC(O)=C2)C1=O
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| InChi Key |
JJXKGUBHEQGADG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13NO3/c1-10-5-6-14-13(7-10)16(15(18)19-14)9-11-3-2-4-12(17)8-11/h2-8,17H,9H2,1H3
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| Chemical Name |
3-[(3-hydroxyphenyl)methyl]-5-methyl-1,3-benzoxazol-2-one
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~180 mg/mL (~705.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (19.59 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 50.0 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: 5 mg/mL (19.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (19.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9176 mL | 19.5879 mL | 39.1757 mL | |
| 5 mM | 0.7835 mL | 3.9176 mL | 7.8351 mL | |
| 10 mM | 0.3918 mL | 1.9588 mL | 3.9176 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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