| dbo:abstract |
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). 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. (en) PP2は、がん研究においてSrcファミリーキナーゼに対する「選択的」阻害剤として頻繁に使用されてきた物質である。PP2は (IC50=4 nM)、 (5 nM)、 (5 nM) を強力に阻害し、上皮成長因子受容体 (EGFR) に対する阻害は弱く (480 nM)、 (100 µM) および (50 µM) に対しては実質的に阻害作用を示さない。Src-選択的阻害剤としての広範な使用にもかかわらず、最近の研究ではPP2が非選択的であり、その他の多くのキナーゼを同様の親和性で阻害することが明らかにされている。 (ja) |
| dbo:iupacName |
1-tert-Butyl-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (en) |
| dbo:thumbnail |
wiki-commons:Special:FilePath/PP2_skeletal.svg?width=300 |
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3927 (xsd:nonNegativeInteger) |
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| dbo:wikiPageWikiLink |
dbr:Epidermal_growth_factor_receptor dbc:Aromatic_amines dbc:Chloroarenes dbr:Molar_concentration dbr:Hck dbc:Protein_kinase_inhibitors dbc:Pyrazolopyrimidines dbr:Lck dbr:Dimethyl_sulfoxide dbr:FYN dbr:IC50 dbr:ZAP-70 dbr:JAK2 dbr:Kinase_inhibitor dbr:Src-family_kinase |
| dbp:imagefile |
PP2 skeletal.svg (en) |
| dbp:imagesize |
120 (xsd:integer) |
| dbp:name |
PP2 (en) |
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1 (xsd:integer) |
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changed (en) |
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changed (en) |
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dbt:Biochemistry-stub dbt:Chembox dbt:Chembox_Hazards dbt:Chembox_Identifiers dbt:Chembox_Properties dbt:Reflist dbt:Cascite dbt:Chemspidercite dbt:Fdacite |
| dct:subject |
dbc:Aromatic_amines dbc:Chloroarenes dbc:Protein_kinase_inhibitors dbc:Pyrazolopyrimidines |
| gold:hypernym |
dbr:Substance |
| rdf:type |
owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q11173 yago:WikicatAromaticAmines yago:Abstraction100002137 yago:AliphaticCompound114601294 yago:Amine114739004 yago:Chemical114806838 yago:Compound114818238 yago:Material114580897 yago:Matter100020827 yago:MethaneSeries114951377 yago:OrganicCompound114727670 yago:Part113809207 yago:PhysicalEntity100001930 yago:Relation100031921 dbo:ChemicalCompound yago:Substance100019613 |
| rdfs:comment |
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). 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. (en) PP2は、がん研究においてSrcファミリーキナーゼに対する「選択的」阻害剤として頻繁に使用されてきた物質である。PP2は (IC50=4 nM)、 (5 nM)、 (5 nM) を強力に阻害し、上皮成長因子受容体 (EGFR) に対する阻害は弱く (480 nM)、 (100 µM) および (50 µM) に対しては実質的に阻害作用を示さない。Src-選択的阻害剤としての広範な使用にもかかわらず、最近の研究ではPP2が非選択的であり、その他の多くのキナーゼを同様の親和性で阻害することが明らかにされている。 (ja) |
| rdfs:label |
PP2 (化合物) (ja) PP2 (kinase inhibitor) (en) |
| owl:sameAs |
freebase:PP2 (kinase inhibitor) yago-res:PP2 (kinase inhibitor) wikidata:PP2 (kinase inhibitor) http://azb.dbpedia.org/resource/پیپی۲_(بازدارنده_کاینیز) dbpedia-fa:PP2 (kinase inhibitor) dbpedia-ja:PP2 (kinase inhibitor) dbpedia-sh:PP2 (kinase inhibitor) dbpedia-sr:PP2 (kinase inhibitor) https://global.dbpedia.org/id/4sqAY |
| prov:wasDerivedFrom |
wikipedia-en:PP2_(kinase_inhibitor)?oldid=1105330964&ns=0 |
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wiki-commons:Special:FilePath/PP2_skeletal.svg |
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wikipedia-en:PP2_(kinase_inhibitor) |
| foaf:name |
PP2 (en) |
| is dbo:wikiPageWikiLink of |
dbr:Src_inhibitor dbr:FYN |
| is foaf:primaryTopic of |
wikipedia-en:PP2_(kinase_inhibitor) |
