Name: AG-490
Price: 196.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    AG-490 is an inhibitor of tyrosine kinases [1].
    As a member of the tyrphostin family, AG-490 is reported to have inhibitory activity against many kinases. It can inhibit the hyperactive JAK2 in B cell precursors of ALL patients, inhibit cytokine-induced activation of JAK2 in eosinophils and suppresses the activation of STAT3 in mycosis fungoides-derived T cells. AG-490 is also found to target JAK3 and its downstream STAT and MAPK signaling pathways. In the IL-2-dependent T cell line, D10, AG-490 suppresses IL-2-induced cell proliferation with IC50 value of 25μM without affecting IL-2R chain expression. It also inhibits IL-2-modulated phosphorylation of STAT5a and STAT5b with IC50 value of 50μM-70μM. Moreover, AG-490 reduces IL-2-induced DNA binding by 78%, 65% and 65% for STAT5a/5b, STAT1 and STAT3, respectively. All these show that AG-490 may provide a beneficial therapeutic by suppressing immunopathological states [1].
    
    [1] Wang L H, Kirken R A, Erwin R A, et al. JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response. The Journal of Immunology, 1999, 162(7): 3897-3904.
- Properties
  - Alternative Name
    
    Tyrphostin B42; (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
    
    CAS Number
    
    133550-30-8
    
    Molecular Formula
    
    C17H14N2O3
    
    Molecular Weight
    
    294.3
    
    Appearance
    
    A solid
    
    Purity
    
    99.51%
    
    Solubility
    
    insoluble in H2O; ≥14.7 mg/mL in DMSO; ≥4.73 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. HONGMEI QU, QUN YU, et al. "HIF-3α affects preeclampsia development by regulating EVT growth via activation of the Flt-1/JAK/STAT signaling pathway in hypoxia." Mol Med Rep. 2021 Jan;23(1):68. PMID:33215219
    2. Fei S, Li W, et al. "Protective Effect of Alprostadil on Acute Pancreatitis in Rats via Inhibiting Janus Kinase 2 (JAK2)/STAT3 Signal Transduction Pathway." Med Sci Monit. 2019 Oct 13;25:7694-7701. PMID:31606729
    3. Xin M, Jin X, et al. "Dipeptidyl peptidase-4 inhibition prevents vascular aging in mice under chronic stress: Modulation of oxidative stress and inflammation." Chem Biol Interact. 2019 Oct 2:108842. PMID:31586451
    4. Zhou H, Sun Y, et al. "Paris saponin VII extracted from trillium tschonoskii suppresses proliferation and induces apoptosis of human colorectal cancer cells." J Ethnopharmacol. 2019 Jul 15;239:111903. PMID:31047966
    5. Lan H, Su Y, et al. "Melatonin protects circulatory death heart from ischemia/reperfusion injury via the JAK2/STAT3 signalling pathway." Life Sci. 2019 Jul 1;228:35-46. PMID:31028804
    6. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
    7. Wang L, Zhang F, et al. "CAFs enhance paclitaxel resistance by inducing EMT through the IL 6/JAK2/STAT3 pathway." Oncol Rep. 2018 May;39(5):2081-2090. PMID:29565447

AG-490

AG-490

Background

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