3-Methyltoxoflavin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE3-MethyltoxoflavinCat. No.: HY-111117CAS No.: 32502-62-8分式: CHNO分量: 207.19作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (723.97 mM; Need ultrasonic)Mass So

2、lvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.8265 mL 24.1324 mL 48.2649 mL5 mM 0.9653 mL 4.8265 mL 9.6530 mL10 mM 0.4826 mL 2.4132 mL 4.8265 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该

3、溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.07 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (12.07 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (12.07 mM); Clear solution

4、1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 3-Methyltoxoflavin蛋质硫键异构酶 (PDI) 的有效抑制剂，其 IC50 值为 170 nM。IC50 & Target IC50: 170 nM (PDI) 1.体外研究 3-Methyltoxoflavin is a potent Protein disulfide isomerase (PDI) inhibitor, with an IC50 of 170 nM. 3-Methyltoxoflavin is toxic in a

5、 panel of human glioblastoma cell lines. From the screen, 3-Methyltoxoflavinemerges as the most cytotoxic inhibitor of PDI. Bromouridine labeling and sequencing (Bru-seq) of nascentRNA reveals that 3-Methyltoxoflavin induces Nrf2 antioxidant response, ER stress response, and autophagy.Specifically,

6、3-Methyltoxoflavin upregulates heme oxygenase 1 and SLC7A11 transcription and proteinexpression and represses PDI target genes such as TXNIP and EGR1. Interestingly, 3-Methyltoxoflavin-induced cell death does not proceed via apoptosis or necrosis, but by a mixture of autophagy and ferroptosis1.PROTO

7、COLCell Assay 1 The colon cancer cells are seeded in duplicate in 96-well plates at 7000-10000 cells per well. For thecombination therapies, NAC is added to the well at the same time as 3-Methyltoxoflavin (35G8) (24 hoursafter plates are seeded), and Z-VAD-FMK and Necrostatin-1 are added to the well

8、 1 hour prior to 3-Methyltoxoflavin addition. Cell growth inhibition is assessed by the cell viability rate. Cell viability isdetermined with the MTT assay. U87MG cells are seeded at 5000 cells per well in 96-well plates.Deferoxamine is added to cells in a five-point, three-fold dilution series from

9、 400 M. 3-Methyltoxoflavin isadded immediately after in a five-point, three-fold dilution series from 100 M. Cells are incubated withcompounds for 12 hours 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kyani A, et al. Discovery and Mechanistic Elucidation of a Class of Protein Disulfide Isomerase Inhibitors for the Treatment ofGlioblastoma. ChemMedChem. 2018 Jan 22;13(2):164-177.McePdfHeightCaution: Product has not been fully validated fo