For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>PP2(AGL 1879) is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases with IC50s of 4/5/5/100 nM for p56lck/p59fynT/Hck/Src respectively.<br>IC50 Value: 4 nM (p56lck); 5 nM (p59fynT); 5 nM (Hck); 100 nM (Src) [1]<br>PP2 inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). PP2 does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 M), or ZAP-70 (IC50 > 100 M). PP2 inhibits the activation of focal adhesion kinase as well as its phosphorylation at Tyr577. PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC50 value of 600 nM [1]. PP2 suppressed cell proliferation and altered cell cycle distribution of the OV1063 cells in a dose- and time-dependent manner. Immunoblotting analysis indicated that PP2 decreased the level of pp60Src protein [2].<br></p>
| Catalog Number | I002249 |
| CAS Number | 172889-27-9 |
| Synonyms | 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine |
| Molecular Formula | C₁₅H₁₆ClN₅ |
| Purity | ≥95% |
| Target | Src |
| Solubility | 25 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 4 nM (p56lck); 5 nM (p59fynT); 5 nM (Hck); 100 nM (Src) [1] |
| InChI | InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19) |
| InChIKey | PBBRWFOVCUAONR-UHFFFAOYSA-N |
| SMILES | CC(C)(C)N1C2=C(C(=N1)C3=CC=C(C=C3)Cl)C(=NC=N2)N |
| Reference | </br>1:The associated pyrazolopyrimidines PP1 and PP2 inhibit protein tyrosine kinase 6 activity and suppress breast cancer cell proliferation. Shim HJ, Kim HI, Lee ST.Oncol Lett. 2017 Mar;13(3):1463-1469. doi: 10.3892/ol.2017.5564. Epub 2017 Jan 2. PMID: 28454278 Free PMC Article</br>2:Genomic characterization of bacteriophage vB_PcaP_PP2 infecting Pectobacterium carotovorum subsp. carotovorum, a new member of a proposed genus in the subfamily Autographivirinae. Lim JA, Heu S, Park J, Roh E.Arch Virol. 2017 Apr 13. doi: 10.1007/s00705-017-3349-6. [Epub ahead of print] PMID: 28409265 </br>3:Knockout of ATG5 leads to malignant cell transformation and resistance to Src family kinase inhibitor PP2. Hwang SH, Han BI, Lee M.J Cell Physiol. 2017 Mar 15. doi: 10.1002/jcp.25912. [Epub ahead of print] PMID: 28294316 </br>4:Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2. Wang Y, Gratzke C, Tamalunas A, Rutz B, Ciotkowska A, Strittmatter F, Herlemann A, Janich S, Waidelich R, Liu C, Stief CG, Hennenberg M.Br J Pharmacol. 2016 Sep 17. doi: 10.1111/bph.13623. [Epub ahead of print] PMID: 27638545 </br>5:N-Acyl Dehydrotyrosines, Tyrosinase Inhibitors from the Marine Bacterium Thalassotalea sp. PP2-459. Deering RW, Chen J, Sun J, Ma H, Dubert J, Barja JL, Seeram NP, Wang H, Rowley DC.J Nat Prod. 2016 Feb 26;79(2):447-50. doi: 10.1021/acs.jnatprod.5b00972. Epub 2016 Jan 29. PMID: 26824128 </br>6:A novel cold-adapted type I pullulanase of Paenibacillus polymyxa Nws-pp2: in vivo functional expression and biochemical characterization of glucans hydrolyzates analysis. Wei W, Ma J, Chen SQ, Cai XH, Wei DZ.BMC Biotechnol. 2015 Oct 19;15:96. doi: 10.1186/s12896-015-0215-z. PMID: 26481143 Free PMC Article</br>7:The Effect of Chemoradiotherapy with SRC Tyrosine Kinase Inhibitor, PP2 and Temozolomide on Malignant Glioma Cells In Vitro and In Vivo. Eom KY, Cho BJ, Choi EJ, Kim JH, Chie EK, Wu HG, Kim IH, Paek SH, Kim JS, Kim IA.Cancer Res Treat. 2016 Apr;48(2):687-97. doi: 10.4143/crt.2014.320. Epub 2015 Jun 4. PMID: 26044161 Free PMC Article</br>8:SCF E3 ligase PP2-B11 plays a positive role in response to salt stress in Arabidopsis. Jia F, Wang C, Huang J, Yang G, Wu C, Zheng C.J Exp Bot. 2015 Aug;66(15):4683-97. doi: 10.1093/jxb/erv245. Epub 2015 Jun 2. PMID: 26041321 Free PMC Article</br>9:GW5074 and PP2 kinase inhibitors implicate nontraditional c-Raf and Lyn function as drivers of retinoic acid-induced maturation. Jensen HA, Bunaciu RP, Varner JD, Yen A.Cell Signal. 2015 Aug;27(8):1666-75. doi: 10.1016/j.cellsig.2015.03.014. Epub 2015 Mar 26. PMID: 25817574 Free PMC Article</br>10:A new set of ESTs from chickpea (Cicer arietinum L.) embryo reveals two novel F-box genes, CarF-box_PP2 and CarF-box_LysM, with potential roles in seed development. Gupta S, Garg V, Bhatia S.PLoS One. 2015 Mar 24;10(3):e0121100. doi: 10.1371/journal.pone.0121100. eCollection 2015. PMID: 25803812 Free PMC Article |
