in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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145<br />
COT k<strong>in</strong>ase (MAP3K8)<br />
Ref. 2003<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-FLGFTYVAP<br />
(150 nM)<br />
Measured product phospho-Ulight-FLGFTYVAP<br />
Detection method LANCE<br />
Reference<br />
Raf-1 <strong>in</strong>hibitor (IC 50 : 12.5 µM)<br />
Jia, Y. et al. (2006) Anal. Biochem., 350: 268-276.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [STE] ❚<br />
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<strong>Cerep</strong><br />
services<br />
Receptors<br />
GCK (MAP4K2)<br />
Ref. 2590<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-FLGFTYVAP<br />
(200 nM)<br />
Measured product phospho-Ulight-FLGFTYVAP<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 4.27 nM)<br />
Katz, P. et al. (1994) J. Biol. Chem., 269: 16802-16809.<br />
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Ion<br />
channels<br />
Transporters<br />
HGK (MAP4K4)<br />
Ref. 3365<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
Organ safety profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-FLGFTYVAP<br />
(50 nM)<br />
Measured product phospho-Ulight-FLGFTYVAP<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 14.9 nM)<br />
Yao, Z. et al. (1999) J. Biol. Chem., 274: 2118-2125.<br />
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K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
MEK1 (MAP2K1)<br />
Ref. 3293<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate ATP + <strong>in</strong>activated ERK 2<br />
(50 nM)<br />
Measured product phospho-ERK 2<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 16 nM)<br />
Kupcho, K.R. et al.(2008) Curr. Chem. Genomics., 1: 43-53.<br />
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Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
MEK1<br />
cellul ar<br />
Ref. 3103 Activator effect<br />
Ref. 3108 Inhibitor effect<br />
Q 3 weeks<br />
Source<br />
A431 cells<br />
Measured product phosphorylation<br />
Detection method AlphaScreen<br />
Activator effect Control EGF (10 nM)<br />
Reference EGF (EC 50 : 0.033 nM)<br />
Inhibitor effect Stimulant EGF (0.3 nM)<br />
Reference MEK1/2 <strong>in</strong>hib. (IC 50 : 116.7 nM)<br />
Janmaat, M.L. et al.(2003) Cl<strong>in</strong>. Cancer. Res., 9: 2316-2326.<br />
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[Solvent] must be kept 0.1%<br />
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Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
MEK5 (MAP2K5)<br />
Ref. 2631<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG<br />
(25 nM)<br />
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />
AGCG<br />
Detection method LANCE<br />
Reference staurospor<strong>in</strong>e (IC 50 : 300 nM)<br />
Sato, Y. et al. (2005) Am. J. Pathol., 166: 49-60.<br />
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Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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