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Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $83 | In Stock | In Stock | |
| 5 mg | $203 | In Stock | In Stock | |
| 10 mg | $307 | In Stock | In Stock | |
| 25 mg | $540 | In Stock | In Stock | |
| 50 mg | $738 | In Stock | In Stock | |
| 100 mg | $977 | - | In Stock |
| Description | Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive. |
| Targets&IC50 | IGF-1:400 nM, NS3-DNA complex:3.6 μM |
| In vitro | Experimentally it is indeed found that AG 538 does not compete with ATP but competes with the IGF-1R substrate. Both AG 538 and I-OMe AG 538 inhibit IGR-1R autophosphorylation in intact cells in a dose-dependent manner. Both compounds inhibit the activation of the downstream targets PKB and Erk2.[1] |
| In vivo | Typical assays used to discover and analyze small molecules that inhibit the hepatitis C virus (HCV) NS3 helicase yield few hits and are often confounded by compound interference. FP-based assay was chosen to screen Sigma's Library of Pharmacologically Active Compounds (LOPAC) for compounds that inhibit NS3-DNA complex formation. Four LOPAC compounds inhibited the FP-based assay: aurintricarboxylic acid (ATA) (IC50=1.4 μM), suramin sodium salt (IC50=3.6 μM), NF 023 hydrate (IC50=6.2 μM) and tyrphostin AG 538 (IC50=3.6 μM).[2] |
| Synonyms | AG 538 |
| Molecular Weight | 297.26 |
| Formula | C16H11NO5 |
| Cas No. | 133550-18-2 |
| Smiles | C(/C(=C/C1=CC(O)=C(O)C=C1)/C#N)(=O)C2=CC(O)=C(O)C=C2 |
| Relative Density. | 1.538 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.5 mg/mL (15.14 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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