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	'''PP2''' is a substance used in cancer research as a selective ] for ]s. It strongly inhibits the kinases ] (]=4 ]), ] (5 nM) and ] (5 nM), shows weaker inhibition of ] (480 nM) and practically no inhibition of ] (100 µM) and ] (50 µM).<ref>{{cite journal\|pmid=8557675\|year=1996\|last1=Hanke\|first1=JH\|last2=Gardner\|first2=JP\|last3=Dow\|first3=RL\|last4=Changelian\|first4=PS\|last5=Brissette\|first5=WH\|last6=Weringer\|first6=EJ\|last7=Pollok\|first7=BA\|last8=Connelly\|first8=PA\|title=Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation\|volume=271\|issue=2\|pages=695–701\|journal=The Journal of biological chemistry}}</ref><ref>{{cite journal\|doi=10.1074/jbc.275.18.13789\|pmid=10788500\|year=2000\|last1=Chen\|first1=JK\|last2=Capdevila\|first2=J\|last3=Harris\|first3=RC\|title=Overexpression of C-terminal Src kinase blocks 14, 15-epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis\|volume=275\|issue=18\|pages=13789–92\|journal=The Journal of biological chemistry}}</ref><ref>{{cite journal\|doi=10.1074/jbc.275.16.11706\|pmid=10766791\|year=2000\|last1=Yoshizumi\|first1=M\|last2=Abe\|first2=J\|last3=Haendeler\|first3=J\|last4=Huang\|first4=Q\|last5=Berk\|first5=BC\|title=Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species\|volume=275\|issue=16\|pages=11706–12\|journal=The Journal of biological chemistry}}</ref><ref>{{cite journal\|doi=10.1210/jc.2002-021278\|pmid=12679489\|year=2003\|last1=Carlomagno\|first1=F\|last2=Vitagliano\|first2=D\|last3=Guida\|first3=T\|last4=Basolo\|first4=F\|last5=Castellone\|first5=MD\|last6=Melillo\|first6=RM\|last7=Fusco\|first7=A\|last8=Santoro\|first8=M\|title=Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo3,4-dpyrimidine (PP2)\|volume=88\|issue=4\|pages=1897–902\|journal=The Journal of clinical endocrinology and metabolism }}</ref>		'''PP2''' is a substance used in cancer research as a selective ] for ]s. It strongly inhibits the kinases ] (]=4 ]), ] (5 nM) and ] (5 nM), shows weaker inhibition of ] (480 nM) and practically no inhibition of ] (100 µM) and ] (50 µM).<ref>{{cite journal\|pmid=8557675\|year=1996\|last1=Hanke\|first1=JH\|last2=Gardner\|first2=JP\|last3=Dow\|first3=RL\|last4=Changelian\|first4=PS\|last5=Brissette\|first5=WH\|last6=Weringer\|first6=EJ\|last7=Pollok\|first7=BA\|last8=Connelly\|first8=PA\|title=Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation\|volume=271\|issue=2\|pages=695–701\|journal=The Journal of biological chemistry\|doi=10.1074/jbc.271.2.695}}</ref><ref>{{cite journal\|doi=10.1074/jbc.275.18.13789\|pmid=10788500\|year=2000\|last1=Chen\|first1=JK\|last2=Capdevila\|first2=J\|last3=Harris\|first3=RC\|title=Overexpression of C-terminal Src kinase blocks 14, 15-epoxyeicosatrienoic acid-induced tyrosine phosphorylation and mitogenesis\|volume=275\|issue=18\|pages=13789–92\|journal=The Journal of biological chemistry}}</ref><ref>{{cite journal\|doi=10.1074/jbc.275.16.11706\|pmid=10766791\|year=2000\|last1=Yoshizumi\|first1=M\|last2=Abe\|first2=J\|last3=Haendeler\|first3=J\|last4=Huang\|first4=Q\|last5=Berk\|first5=BC\|title=Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species\|volume=275\|issue=16\|pages=11706–12\|journal=The Journal of biological chemistry}}</ref><ref>{{cite journal\|doi=10.1210/jc.2002-021278\|pmid=12679489\|year=2003\|last1=Carlomagno\|first1=F\|last2=Vitagliano\|first2=D\|last3=Guida\|first3=T\|last4=Basolo\|first4=F\|last5=Castellone\|first5=MD\|last6=Melillo\|first6=RM\|last7=Fusco\|first7=A\|last8=Santoro\|first8=M\|title=Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo3,4-dpyrimidine (PP2)\|volume=88\|issue=4\|pages=1897–902\|journal=The Journal of clinical endocrinology and metabolism }}</ref>

	==References==		==References==

Revision as of 21:09, 20 October 2011

PP2 (kinase inhibitor)
Names

IUPAC name (4-amino-5-(4-chlorophenyl)-7-(dimethylethyl)pyrazolopyrimidine
Identifiers
CAS Number	172889-27-9
3D model (JSmol)	Interactive image
PubChem CID	4878
CompTox Dashboard (EPA)	DTXSID60274447
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)
SMILES Nc2ncnc(c12)n(C(C)(C)C)nc1-c3ccc(Cl)cc3
Properties
Chemical formula	C₁₅H₁₆ClN₅
Molar mass	301.774
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 , 100 kPa). Y verify (what is ?) Infobox references

Chemical compound

PP2 is a substance 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).

References

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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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.

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