PP2
Catalog #:
IN0049| IN0049-1mg | USD99.0 |
| IN0049-5mg | USD384.0 |
Synonyms: PP2
IUPAC Name:
3-(4-chlorophenyl) 1-(1,1-dimethylethyl)-1H-pyrazolo[3 ,4-d]pyrimidin-4-amineFunctional Activity:
PP2 is a substance used in cancer research as a selective inhibitor for Src-family kinases with >10,000-fold selectivity over ZAP-70 and JAK2. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 μM) and JAK2 (50 μM)Technical Data:
M.Wt: 301.78
Formula: C15H16ClN5
Solubility: Soluble to 25 mM in DMSO and to 10 mM in ethanol
Purity: >97%
Storage: Store at 4 degree C
CAS No.: 172889-27-9
Related Products by Target:
Solubility: Soluble to 25 mM in DMSO and to 10 mM in ethanol
Purity: >97%
Storage: Store at 4 degree C
CAS No.: 172889-27-9
Related Products by Target:
Storage: Store at 4 degree C
CAS No.: 172889-27-9
Related Products by Target:
Related Products by Target:
References for PP2:
1. Ahn, J. H. and Lee, M. Suppression of autophagy sensitizes multidrug resistant cells towards Src tyrosine kinase specific inhibitor PP2. Cancer Lett, 310: 188-197.
2. Kong, L., Deng, Z., Shen, H., and Zhang, Y. Src family kinase inhibitor PP2 efficiently inhibits cervical cancer cell proliferation through down-regulating phospho-Src-Y416 and phospho-EGFR-Y1173. Mol Cell Biochem, 348: 11-19.
3. Hishiki, T., Saito, T., Sato, Y., Mitsunaga, T., Terui, E., Matsuura, G., Saito, E., Shibata, R., Mise, N., Yokoyama, Y., and Yoshida, H. Src kinase family inhibitor PP2 induces aggregation and detachment of neuroblastoma cells and inhibits cell growth in a PI3 kinase/Akt pathway-independent manner. Pediatr Surg Int, 27: 225-230.
4. Liu, X., Feng, R., and Du, L. The role of enoyl-CoA hydratase short chain 1 and peroxiredoxin 3 in PP2-induced apoptosis in human breast cancer MCF-7 cells. FEBS Lett, 584: 3185-3192.
5. Schuster, I. G., Busch, D. H., Eppinger, E., Kremmer, E., Milosevic, S., Hennard, C., Kuttler, C., Ellwart, J. W., Frankenberger, B., Nossner, E., Salat, C., Bogner, C., Borkhardt, A., Kolb, H. J., and Krackhardt, A. M. Allorestricted T cells with specificity for the FMNL1-derived peptide PP2 have potent antitumor activity against hematologic and other malignancies. Blood, 110: 2931-2939, 2007.
6. Chiang, G. J., Billmeyer, B. R., Canes, D., Stoffel, J., Moinzadeh, A., Austin, C. A., Kosakowski, M., Rieger-Christ, K. M., Libertino, J. A., and Summerhayes, I. C. The src-family kinase inhibitor PP2 suppresses the in vitro invasive phenotype of bladder carcinoma cells via modulation of Akt. BJU Int, 96: 416-422, 2005.
7. Calcagno, A. M., Fostel, J. M., Orchekowski, R. P., Alston, J. T., Mattes, W. B., Siahaan, T. J., and Ware, J. A. Modulation of cell adhesion molecules in various epithelial cell lines after treatment with PP2. Mol Pharm, 2: 170-184, 2005.
8. Lee, M., Kim, J. Y., and Koh, W. S. Apoptotic effect of PP2 a Src tyrosine kinase inhibitor, in murine B cell leukemia. J Cell Biochem, 93: 629-638, 2004.
9. Carlomagno, F., Vitagliano, D., Guida, T., Basolo, F., Castellone, M. D., Melillo, R. M., Fusco, A., and Santoro, M. Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2). J Clin Endocrinol Metab, 88: 1897-1902, 2003.
10. Nam, J. S., Ino, Y., Sakamoto, M., and Hirohashi, S. Src family kinase inhibitor PP2 restores the E-cadherin/catenin cell adhesion system in human cancer cells and reduces cancer metastasis. Clin Cancer Res, 8: 2430-2436, 2002.
