| Size | Price | Stock | Qty |
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| 5mg |
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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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| Other Sizes |
| Targets |
ERK1/2
Protein tyrosine kinases (inhibitor) Mitogen-activated protein kinase p42MAPK (ERK2) (prevents activation) [1] |
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| ln Vitro |
AG126 (10 μM; overnight) increases the ARPE-19 cells' viability[2].
AG126 at concentrations greater than 10 μM , they become toxic to ARPE-19 cells and can increase the toxicity of H2O2[2]. AG126 (0.1-100 μM) blocks the growth of BRMECs that is induced by VEGF[4] Tyrphostin AG126 prevents the activation of mitogen-activated protein kinase p42MAPK (ERK2). [1] In cultured cells, Tyrphostin AG126 inhibits the phosphorylation of tyrosine residues in proteins induced by inflammatory stimuli, thereby preventing the expression of inducible nitric oxide synthase (iNOS). [1] Tyrphostin AG126 also mediates the inhibition of the inducible isoform of cyclooxygenase-2 (COX-2) expression caused by endotoxin or pro-inflammatory cytokines in murine macrophages and human epithelial cell lines. [1] |
| ln Vivo |
AG 126 (intraperitoneal injection; 1-10 mg/kg; 1 h and 6 h after Zymosan treatment) treatment decreases the severity of multiple organ failure (MOF) brought on by Zymosan-induced peritonitis in rats[3].
In a carrageenan-induced pleurisy model in rats, intraperitoneal administration of Tyrphostin AG126 (1, 3, or 10 mg/kg) significantly reduced pleural exudate volume, polymorphonuclear leukocyte infiltration, and levels of TNF-α and IL-1β in the exudate in a dose-dependent manner. [1] Tyrphostin AG126 also reduced nitrite/nitrate levels (indicator of NO synthesis) and iNOS activity in the lungs of carrageenan-treated rats. [1] In a collagen-induced arthritis model in rats, Tyrphostin AG126 (5 mg/kg i.p. every 48 hours) significantly reduced the incidence and severity of arthritis, paw swelling, bone resorption, osteophyte formation, and plasma levels of TNF-α and IL-1β. [1] Immunohistochemical analysis showed that Tyrphostin AG126 reduced the expression of iNOS, COX-2, nitrotyrosine, and poly(ADP-ribose) polymerase (PARP) in lung tissues (pleurisy model) and joint tissues (arthritis model). [1] |
| Enzyme Assay |
The calcium-independent conversion of L-arginine to L-citrulline in homogenates of pleural macrophages or lungs served as an indicator of iNOS activity. Homogenates were incubated with [³H]-L-arginine, NADPH, calmodulin, tetrahydrobiopterin, and EGTA for 20 minutes at 22°C. Reactions were stopped with ice-cold HEPES buffer containing EGTA and EDTA, and [³H]-L-citrulline was separated using Dowex 50W columns and measured by scintillation counting. [1]
Cyclooxygenase (COX) activity was assessed in lung homogenates by incubating with excess arachidonic acid at 37°C for 30 minutes. The concentration of 6-keto-prostaglandin-F₁α in the supernatant was measured by radioimmunoassay. [1] |
| Cell Assay |
Immunohistochemical localization of iNOS, COX-2, nitrotyrosine, and PARP was performed on lung and joint tissue sections. Tissues were fixed, embedded in paraffin, sectioned, deparaffinized, and treated with hydrogen peroxide to quench endogenous peroxidase. Sections were permeabilized, blocked with normal serum, incubated with primary antibodies overnight, and detected using biotin-conjugated secondary antibodies and avidin-biotin peroxidase complex. [1]
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| Animal Protocol |
Male Sprague-Dawley rats treated with Zymosan (500 mg/kg)[3]
10 mg/kg, 3 mg/kg or 1 mg/kg Intraperitoneal injection; 10, 3, or 1 mg/kg; 1 h and 6 h after Zymosan treatment Carrageenan-induced pleurisy model: Male Sprague-Dawley rats (160–180 g) were used. Tyrphostin AG126 was dissolved in ethanol (final concentration 1%) and administered intraperitoneally as a bolus injection at doses of 1, 3, or 10 mg/kg, 15 minutes before intrapleural injection of carrageenan. Control groups received vehicle (ethanol) or saline. Animals were sacrificed 4 hours after carrageenan injection, and pleural exudate and lung tissues were collected for analysis. [1] Collagen-induced arthritis model: Lewis rats were immunized with bovine type II collagen in complete Freund's adjuvant on day 1 and boosted on day 21. Tyrphostin AG126 (5 mg/kg) was administered intraperitoneally every 48 hours starting from day 24. Arthritis was assessed clinically and histologically until day 35. [1] |
| References |
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| Additional Infomation |
2-[(3-hydroxy-4-nitrophenyl)methylene]malonium is a nitrophenol. Tyrosine kinase inhibitor AG 126 belongs to the tyrosine kinase inhibitor family and can effectively block the production of tumor necrosis factor-α and nitric oxide in lipopolysaccharide-induced macrophages. (NCI)
Tyrosine kinase inhibitor AG 126 is a derivative of benzylmalonium and belongs to the tyrosine kinase inhibitor family. [1] It exerts anti-inflammatory effects by inhibiting the expression of pro-inflammatory cytokines (TNF-α, IL-1β), iNOS, COX-2, and PARP activation, thereby reducing oxidative stress and nitrosation stress in acute and chronic inflammation models. [1] This study suggests that inhibiting protein tyrosine kinases may represent a new approach to treating inflammatory diseases. [1] |
| Molecular Formula |
C₁₀H₅N₃O₃
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|---|---|
| Molecular Weight |
215.17
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| Exact Mass |
215.033
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| Elemental Analysis |
C, 55.82; H, 2.34; N, 19.53; O, 22.31
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| CAS # |
118409-62-4
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| Related CAS # |
118409-62-4
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| PubChem CID |
2046
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
381.9±42.0 °C at 760 mmHg
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| Melting Point |
184 °C
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| Flash Point |
184.8±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
1.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
388
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#C/C(C#N)=C/C1=CC=C([N+]([O-])=O)C(O)=C1
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| InChi Key |
DUQADSPERJRQBW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H5N3O3/c11-5-8(6-12)3-7-1-2-9(13(15)16)10(14)4-7/h1-4,14H
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| Chemical Name |
2-[(3-hydroxy-4-nitrophenyl)methylidene]propanedinitrile
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| Synonyms |
AG 126; AG126; AG-126; UNII-7YA4AMD1JC; Tyrphostin A 10; Tyrphostin AG 126; Tyrphostin A 10; alpha-Cyano-(3-hydroxy-4-nitro)cinnamonitrile
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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 |
| 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: 43~100 mg/mL (199.9~464.8 mM)
Ethanol: ~2 mg/mL (~9.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6475 mL | 23.2374 mL | 46.4749 mL | |
| 5 mM | 0.9295 mL | 4.6475 mL | 9.2950 mL | |
| 10 mM | 0.4647 mL | 2.3237 mL | 4.6475 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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