Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
3-Methyltoxoflavin is a novel inhibitor of Hsp90. 3-Methyltoxoflavin decreases the levels of the Hsp90-dependent client protein HER2, with associated cell death.
ln Vitro |
3-Mmethyltoxoflavin has an IC50 of 170 nM, making it a strong inhibitor of protein disulfide isomerase (PDI). 3. Human glioblastoma cell lines are susceptible to the toxicity of methyltoxin. The most cytotoxic PDI inhibitor, according to the screening results, is 3-methyltoxin. The induction of Nrf2 antioxidant response, endoplasmic reticulum stress response, and autophagy was demonstrated by 3-methyltoxoflavin using bru-seq (bromouridine labeling and sequencing) of nascent RNA. More precisely, 3-Mmethyltoxoflavin suppresses PDI target genes like TXNIP and EGR1 while upregulating heme oxygenase 1 and SLC7A11 transcription and protein expression. Remarkably, a combination of autophagy and ferroptosis rather than apoptosis or necrosis drives the process of 3-methyltoxin-induced cell death [1].
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References |
[1]. Kyani A, et al. Discovery and Mechanistic Elucidation of a Class of Protein Disulfide Isomerase Inhibitors for the Treatment of Glioblastoma. ChemMedChem. 2018 Jan 22;13(2):164-177
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Molecular Formula |
C8H9N5O2
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Molecular Weight |
207.193
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Exact Mass |
207.0756
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CAS # |
32502-62-8
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Related CAS # |
32502-62-8
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SMILES |
CC1=NN(C)C(C2=N1)=NC(N(C)C2=O)=O
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InChi Key |
CPXHNWKHOFNPDO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C8H9N5O2/c1-4-9-5-6(13(3)11-4)10-8(15)12(2)7(5)14/h1-3H3 S
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Chemical Name |
1,3,6-Trimethyl-pyrimido[5,4-e]-1,2,4-triazine-5,7(1H,6H)-dione
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Synonyms |
3-Methyltoxoflavin 3 Methyltoxoflavin 3Methyltoxoflavin GNF-Pf-2272.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 : ~50 mg/mL (~241.32 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (24.13 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 (24.13 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear 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: ≥ 2.5 mg/mL (12.07 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 | 4.8265 mL | 24.1324 mL | 48.2649 mL | |
5 mM | 0.9653 mL | 4.8265 mL | 9.6530 mL | |
10 mM | 0.4826 mL | 2.4132 mL | 4.8265 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.