Replaces Prod. #: ALX-270-168
AG-490 is a potent inhibitor of the JAK-2 tyrosine kinase. In acute lymphoblastic leukemia (ALL) cells, which abundantly express JAK-2, AG-490 dose-dependently inhibited DNA synthesis, blocked cell growth and induced apoptosis. At 5 µM, AG-490 almost completely blocked the growth of all pre-B ALL cells but had no significant effect on the growth of mitogen-stimulated normal B or T cells, B-cell lymphoma or T-cell leukemia cells. AG-490 does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src. It blocks interleukin-7-induced JAK kinase activity in T-cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. AG-490 is cell permeable and is a valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Details
Alternative Name: | N-Benzyl-3,4-dihydroxybenzylidenecyanoacetamide |
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Formula: | C17H14N2O3 |
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MW: | 294.3 |
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CAS: | 133550-30-8 |
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Purity: | ≥98% (TLC) |
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Appearance: | Tan solid. |
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Solubility: | Soluble in DMSO (30mg/ml), dimethyl formamide (40mg/ml) or 100% ethanol (10mg/ml). |
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Shipping: | Ambient Temperature |
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Long Term Storage: | -20°C |
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Use/Stability: | Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 2 months. |
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Handling: | Protect from light. |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells: J. De Vos, et al.; Br. J. Haematol.
109, 823 (2000),
Abstract;
JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response: L.H. Wang, et al.; J. Immunol.
162, 3897 (1999),
Abstract;
Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells: R.A. Kirken, et al.; J. Leukoc. Biol.
65, 891 (1999),
Abstract;
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature
379, 645 (1996),
Abstract;
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood
86, 2077 (1995),
Abstract;
Activation of phosphatidylinositol-3 kinase by ligation of the interleukin-7 receptor is dependent on protein tyrosine kinase activity: H. Dadi, et al.; Blood
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Abstract;
Tyrphostins--potential antiproliferative agents and novel molecular tools: A. Levitzki; Biochem. Pharmacol.
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Abstract;
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem.
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Abstract;