PP2 (kinase inhibitor)

PP2
Names
Preferred IUPAC name
1-tert-Butyl-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Identifiers
3D model (JSmol)
ChEBI
ChemSpider
UNII
  • 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)
  • Nc2ncnc(c12)n(C(C)(C)C)nc1-c3ccc(Cl)cc3
Properties
C15H16ClN5
Molar mass 301.78 g·mol−1
Appearance White to off-white solid
Solubility in DMSO 25 mg/ml
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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PP2 is a substance that has frequently been used in cancer research as a "selective" inhibitor for Src-family kinases. 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).[1][2][3][4] Despite its extensive use as a Src-selective inhibitor, recent research has shown that PP2 is non-selective and inhibits many other kinases with similar affinities.[5]

References

  1. ^ Hanke, JH; Gardner, JP; Dow, RL; Changelian, PS; Brissette, WH; Weringer, EJ; Pollok, BA; Connelly, PA (1996). "Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation". The Journal of Biological Chemistry. 271 (2): 695–701. doi:10.1074/jbc.271.2.695. PMID 8557675.
  2. ^ Chen, JK; Capdevila, J; Harris, RC (2000). "Overexpression of C-terminal Src kinase blocks 14, 15-epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis". The Journal of Biological Chemistry. 275 (18): 13789–92. doi:10.1074/jbc.275.18.13789. PMID 10788500.
  3. ^ Yoshizumi, M; Abe, J; Haendeler, J; Huang, Q; Berk, BC (2000). "Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species". The Journal of Biological Chemistry. 275 (16): 11706–12. doi:10.1074/jbc.275.16.11706. PMID 10766791.
  4. ^ Carlomagno, F; Vitagliano, D; Guida, T; Basolo, F; Castellone, MD; Melillo, RM; Fusco, A; Santoro, M (2003). "Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo3,4-dpyrimidine (PP2)". The Journal of Clinical Endocrinology and Metabolism. 88 (4): 1897–902. doi:10.1210/jc.2002-021278. PMID 12679489.
  5. ^ Brandvold, KR; Steffey, ME; Fox, CC; Soellner, MB (2012). "Development of a Highly Selective c-Src Kinase Inhibitor". ACS Chemical Biology. ASAP (8): 1393–1398. doi:10.1021/cb300172e. PMC 3423592. PMID 22594480.


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