PP1

CHF 60.00
In stock
AG-CR1-3562-M0011 mgCHF 60.00
AG-CR1-3562-M0055 mgCHF 190.00
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Product Details
Synonyms 4-Amino-5-(methylphenyl)-7-(tert.butyl)pyrazolo-(3,4-d)pyrimidine
Product Type Chemical
Properties
Formula

C16H19N5

MW 281.4
CAS 172889-26-8
Purity Chemicals ≥98% (HPLC)
Appearance White solid.
Solubility Soluble in DMSO. Slightly soluble in ethanol.
InChi Key ZVPDNRVYHLRXLX-UHFFFAOYSA-N
Smiles CC1=CC=C(C=C1)C1=NN(C2=C1C(N)=NC=N2)C(C)(C)C
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Working aliquots are stable for up to 3 months when stored at -20°C.
Documents
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Product Specification Sheet
Datasheet Download PDF
Description
  • Highly potent and selective Scr family tyrosine kinase inhibitor [1, 2, 6, 9].
  • Shows anti-Ras cancer potential by blocking Ras-induced activation of PAK1 [4].
  • Antitumor compound [3, 4, 5, 7]. 
  • RIP2 inhibitor [9].
  • Blocks TGF-β-mediated cellular responses [8, 10].
Product References
  1. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation: J.H. Hanke, et al.; J. Biol. Chem. 271, 695 (1996)
  2. Src family-selective tyrosine kinase inhibitor, PP1, inhibits both Fc epsilonRI- and Thy-1-mediated activation of rat basophilic leukemia cells: M. Amoui, et al.; Eur. J. Immunol. 27, 1881 (1997) 
  3. Lck associates with and is activated by Kit in a small cell lung cancer cell line: inhibition of SCF-mediated growth by the Src family kinase inhibitor PP1: G.W. Krystal, et al.; Cancer Res. 58, 4660 (1998)
  4. An anti-Ras cancer potential of PP1, an inhibitor specific for Src family kinases: in vitro and in vivo studies: H. He, et al.; Cancer J. 6, 243 (2000)
  5. The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes: F. Carlomagno, et al.; Cancer Res. 62, 1077 (2002)
  6. The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003)
  7. The Src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases: L. Tatton, et al.; J. Biol. Chem. 278, 4847 (2003)
  8. Src activation is not necessary for transforming growth factor (TGF)-beta-mediated epithelial to mesenchymal transitions (EMT) in mammary epithelial cells. PP1 directly inhibits TGF-beta receptors I and II: M. Maeda, et al.; J. Biol. Chem. 281, 59 (2006)
  9. The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007)
  10. The Src family kinase inhibitors PP2 and PP1 block TGF-beta1-mediated cellular responses by direct and differential inhibition of type I and type II TGF-beta receptors: H. Ungefroren, et al.; Curr. Cancer Drug Targets 11, 524 (2011)
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