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Janus Kinases [JAKs] / Related Products
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ALX-270-168 Revised 18-May-06
Tyrphostin AG 490
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SYNONYMS Tyrphostin B42
N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-]N-benzylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-168-M005   5 mg 45.00 USD Add To Cart
ALX-270-168-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2O3
MW: 294.3
CAS NUMBER: 133550-30-8
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO and acetone; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selectively inhibits CDK2 activation leading to a potent cell cycle arrest at late G1 and S phase. Cell permeable inhibitor of JAK-2 tyrosine kinase. Does not significantly inhibit other kinases, such as Lck, Lyn, Btk, Syk or Src. Blocks IL-7 induced JAK kinase activity in T cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. Valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Specific Literature References
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989) Abstract
Tyrosine phosphorylation is an obligatory event in IL-2 secretion [published erratum appears in J Immunol 1991 May 1;146(9):3260]: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990) 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; Full Text
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood 86, 2077 (1995) Abstract; Full Text
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature 379, 645 (1996) 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
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
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
Further Categories Containing This Product:
Janus Kinases [JAKs] / Related Products • Tyrosine Kinase Inhibitors • CDK & Cyclin Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
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