AG490

Name Value
Weight 294.310 g/mol
Zinc ID ZINC12352668
Smiles N#C/C(=C/c1ccc(O)c(O)c1)C(=O)NCc1ccccc1
Molecular formula C17H14N2O3
Mode of inhibition JAK2, JAK3, STAT; Tyrosine kinase inhibitor
CAS 133550-30-8

Clinical Trials

Study title Status Conditions Link

References

Publication DOI Pubmed PMCID
Janus Kinase 2 Inhibitor AG490 Inhibits the STAT3 Signaling Pathway by Suppressing Protein Translation of gp130. 10.4196/kjpp.2009.13.2.131 https://www.ncbi.nlm.nih.gov/pubmed/19885008 N/A
JAK inhibitors AG-490 and WHI-P154 decrease IFN-gamma-induced iNOS expression and NO production in macrophages. Mediators of inflammation Outi Sareila, Riku Korhonen, Outi Kärpänniemi, Riina Nieminen, Hannu Kankaanranta, Eeva Moilanen, 2006, 2, None, None, 10.1155/MI/2006/16161 10.1155/MI/2006/16161 16883061 PMC1592588
AG490 suppresses EPO-mediated activation of JAK2-STAT but enhances blood flow recovery in rats with critical limb ischemia. Journal of inflammation (London, England) Han-Tan Chai, Hon-Kan Yip, Cheuk-Kwan Sun, Shu-Yuan Hsu, Steve Leu, 13, None, None, 2016-06-04, 10.1186/s12950-016-0126-3 10.1186/s12950-016-0126-3 27274711 PMC4893245
Effects of IL-6 and AG490 on regulation of Stat3 signaling pathway and invasion of human pancreatic cancer cells in vitro. Journal of experimental & clinical cancer research : CR Chen Huang, Guang Yang, Tao Jiang, Kejian Huang, Jun Cao, Zhengjun Qiu, 29, None, 2010-05-19, 2010-05-19, 10.1186/1756-9966-29-51 10.1186/1756-9966-29-51 20482858 PMC2883975
High mobility group box 1 induces the activation of the Janus kinase 2 and signal transducer and activator of transcription 3 (JAK2/STAT3) signaling pathway in pancreatic acinar cells in rats, while AG490 and rapamycin inhibit their activation. Bosnian journal of basic medical sciences Guoliang Wang, Jingchao Zhang, Danhua Dui, Haoyuan Ren, Jin Liu, 16, 4, 2016-11-10, 2016-11-10, 10.17305/bjbms.2016.1442 10.17305/bjbms.2016.1442 27754827 PMC5136768
AG490 ameliorates early brain injury via inhibition of JAK2/STAT3-mediated regulation of HMGB1 in subarachnoid hemorrhage. Experimental and therapeutic medicine Ji-Yang An, Hong-Gang Pang, Ting-Qin Huang, Jin-Ning Song, Dan-Dong Li, Yong-Lin Zhao, Xu-Dong Ma, 15, 2, None, 2017-11-22, 10.3892/etm.2017.5539 10.3892/etm.2017.5539 29434719 PMC5774435

Vendors

Company Lnk to product
InvivoGen https://www.invivogen.com/ag490
Tocris https://www.tocris.com/products/ag-490_0414
Selleckchem https://www.selleckchem.com/products/AG-490.html
MedChemExpress https://www.medchemexpress.com/AG-490.html
MERCK (Sigma Aldrich) https://www.sigmaaldrich.com/catalog/product/mm/658401?lang=pl&region=PL
TargetMol https://www.targetmol.com/compound/AG-490
Axon Medchem https://www.axonmedchem.com/product/1378
Caymanchemical https://www.caymanchem.com/product/10010311/ag-490
BLDpharm https://www.bldpharm.com/products/133550-30-8.html

Filter data

Compound AG490
Experiment types Griess reaction, Hematoxylin and eosin staining , Immunocytochemistry, Immunofluorescence, Immunohistochemical staining, Invasion assay , Laser Doppler, Luciferase promoter assay, MMT, RT-PCR, RT-qPCR, TUNEL, Western Blot
Concentrations 1.00, 10.00, 100.00, 20.00, 25.00, 3.00, 30.00, 5.00, 50.00
Cell lines 1774 macrophages, Brain tissue , Pancreatic Acinar Cells , RT4, SW1990, quadriceps
Organisms Homo sapiens, Rattus norvegicus
Animal models Sprague-Dawley (SD) rats
STAT proteins STAT1, STAT1α, STAT3, STAT5, p-STAT1, p-STAT3, p-STAT5
Other Akt, Bax, Bcl-2, Caspase-3, ERK1/2, GADD, GAPDH, GPx, GR, HMGB1, HMGB1 (cytoplasm), HMGB1 (nucleus), HO-1, IL-10, JAK2, JNK, LMNB1, MMP-2, NF-κB, NOQ1, TNF-α, Unc5b, VEGF, gp130, iNOS, p-Akt, p-ERK1/2, p-JAK2, p-JNK, peIF2a, β-actin, β-tubulin

Experiments

Compound Experiment type Investigated event Concentration Cell line Organism Animal model Stat protein Details
AG490 Western Blot Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens p-STAT3
AG490 Western Blot Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens STAT3
AG490 Western Blot Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens
AG490 Luciferase promoter assay Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity in presence of IL-6 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 1.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 5.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 20.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 100.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 1.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 5.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 20.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 100.00 µM RT4 Homo sapiens
AG490 RT-PCR Influence on gene expression levels 50.00 µM RT4 Homo sapiens
AG490 RT-PCR Influence on gene expression levels 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein degradation 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity in presence of protease inhibitors 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity in presence of protease inhibitors 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein synthesis 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein synthesis 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influene on protein activity in presence of ER stress inducer 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influene on protein activity in presence of ER stress inducer 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influene on protein activity in presence of ER stress inducer 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on correlation between proetin levels and IL-6 response 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on correlation between proetin levels and IL-6 response 50.00 µM RT4 Homo sapiens p-STAT3
AG490 Western Blot Influence on correlation between proetin levels and IL-6 response 50.00 µM RT4 Homo sapiens STAT3
AG490 Western Blot Influence on correlation between proetin levels and IL-6 response 50.00 µM RT4 Homo sapiens
AG490 Western Blot Influence on protein activity in presence of IFNγ 10.00 µM 1774 macrophages Homo sapiens STAT1α
AG490 Western Blot Influence on protein activity in presence of IFNγ 100.00 µM 1774 macrophages Homo sapiens STAT1α
AG490 Griess reaction Influence on nitric oxide (NO) generation 3.00 µM 1774 macrophages Homo sapiens
AG490 Griess reaction Influence on nitric oxide (NO) generation 10.00 µM 1774 macrophages Homo sapiens
AG490 Griess reaction Influence on nitric oxide (NO) generation 30.00 µM 1774 macrophages Homo sapiens
AG490 Western Blot Influence on protein activity in presence of IFNγ 3.00 µM 1774 macrophages Homo sapiens
AG490 Western Blot Influence on protein activity in presence of IFNγ 10.00 µM 1774 macrophages Homo sapiens
AG490 RT-qPCR Influence on gene expression levels in presence of IFNγ 10.00 µM 1774 macrophages Homo sapiens
AG490 RT-qPCR Influence on gene expression levels in presence of IFNγ 10.00 µM 1774 macrophages Homo sapiens
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats p-STAT1
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats STAT1
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats p-STAT3
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats STAT3
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats p-STAT5
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats STAT5
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 TUNEL Influence on EPO administration and apoptosis 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Hematoxylin and eosin staining Influence on EPO in ischemic quadriceps 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR Influence on gene expression levels in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Immunohistochemical staining Influence on EPOR activity in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Laser Doppler Influence on blood flow recovery in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Immunohistochemical staining Influence on vessel density in presence of CLI and/or EPO 3.00 mg/kg quadriceps Rattus norvegicus Sprague-Dawley (SD) rats
AG490 MMT Influence on cell viability 20.00 µM SW1990 Homo sapiens
AG490 RT-qPCR Influence on gene expression levels 20.00 µM SW1990 Homo sapiens
AG490 RT-qPCR Influence on gene expression levels 20.00 µM SW1990 Homo sapiens
AG490 Immunocytochemistry Influence on protein activity 20.00 µM SW1990 Homo sapiens STAT3
AG490 Western Blot Influence on protein activity 20.00 µM SW1990 Homo sapiens p-STAT3
AG490 Western Blot Influence on protein activity 20.00 µM SW1990 Homo sapiens STAT3
AG490 Western Blot Influence on protein activity 20.00 µM SW1990 Homo sapiens
AG490 Western Blot Influence on protein activity 20.00 µM SW1990 Homo sapiens
AG490 Western Blot Influence on protein activity 20.00 µM SW1990 Homo sapiens
AG490 Invasion assay Influence on cell motility 20.00 µM SW1990 Homo sapiens
AG490 Western Blot 25.00 μM/L Pancreatic Acinar Cells Rattus norvegicus Sprague-Dawley (SD) rats STAT3
AG490 Western Blot 25.00 μM/L Pancreatic Acinar Cells Rattus norvegicus Sprague-Dawley (SD) rats
AG490 RT-qPCR 25.00 μM/L Pancreatic Acinar Cells Rattus norvegicus Sprague-Dawley (SD) rats STAT3
AG490 RT-qPCR 25.00 μM/L Pancreatic Acinar Cells Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats p-STAT3
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats STAT3
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein activity in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein motility in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein motility in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein motility in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Western Blot Influence on protein motility in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 Immunofluorescence Influence on protein motility in presence of SAH 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats
AG490 TUNEL Influence on neuronal apoptosis 10.00 µM Brain tissue Rattus norvegicus Sprague-Dawley (SD) rats