AG-490

JAK inhibitor



BML-EI272-0010	10 mg	110.00 USD

BML-EI272-0050	50 mg	443.00 USD
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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

Formula:	C₁₇H₁₄N₂O₃

MW:	294.3

CAS:	133550-30-8

Purity:	≥98% (TLC)

Appearance:	Tan solid.

Solubility:	Soluble in DMSO (30mg/ml), dimethyl formamide (40mg/ml) or 100% ethanol (10mg/ml).

Shipping:	Ambient Temperature

Long Term Storage:	-20°C

Use/Stability:	Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 2 months.

Handling:	Protect from light.

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 84, 1579 (1994), Abstract;

Tyrphostins--potential antiproliferative agents and novel molecular tools: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990), Abstract;

Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989), Abstract;