in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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151<br />
RAF-1/MEK1<br />
Ref. 1703<br />
Q 3 weeks<br />
RIPK2<br />
Ref. 2763<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 (<strong>in</strong>sect cells)<br />
Substrate ATP + <strong>in</strong>active MEK1<br />
(200 nM)<br />
Measured product phospho-ERK 2<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 150 nM)<br />
Force, T. et al. (1994) Proc. Natl. Acad. Sci. USA, 91: 1270-1274.<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG<br />
-9 -8 -7 -6 -5 -4<br />
(25 nM)<br />
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />
AGCG<br />
Detection method LANCE<br />
Reference staurospor<strong>in</strong>e (IC 50 : 150 nM)<br />
McCarthy, J.V. et al. (1998) J. Biol. Chem., 273: 16968-16975.<br />
-10<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [TKL] ❚<br />
enzyme activity (% of control)<br />
<br />
100<br />
50<br />
0<br />
-11<br />
<br />
-10<br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
-10 -9 -8 -7 -6 -5 -4<br />
-9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5<br />
<br />
-10 -9 -8 -7 -6 -5<br />
<br />
<br />
-3<br />
<br />
staurospor<strong>in</strong>e<br />
ZM336372<br />
PD98059<br />
U0126<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
Ion<br />
channels<br />
Transporters<br />
TAK1-TAB1 (MAP3K7)<br />
Ref. 3017<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 : 95 nM)<br />
Safwat, N. et al. (2005) Endocr<strong>in</strong>ol., 146: 4814-4824.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
<br />
❚ other k<strong>in</strong>ases<br />
<br />
<br />
<br />
<br />
Other<br />
enzymes<br />
AurA/Aur2 k<strong>in</strong>ase<br />
Ref. 2885<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant (Sf21 cells)<br />
Substrate ATP + Ulight-RRRSLLE<br />
(100 nM)<br />
Measured product phospho-Ulight-RRRSLLE<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 10 nM)<br />
Sun, C. et al. (2004) J. Biomol. Screen., 9: 391-397.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Specialized<br />
cellular<br />
assays<br />
Standard<br />
profiles<br />
AurB/Aur1 k<strong>in</strong>ase<br />
Ref. 1841<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 (<strong>in</strong>sect cells)<br />
Substrate ATP + biot<strong>in</strong>yl-PLK-derived peptide<br />
(50 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-PLK-derived peptide<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 46 nM)<br />
Bishop, J.D. and Schumacher, J.M. (2002) J. Biol. Chem., 277: 27577-27580.<br />
enzyme activity (% of control)<br />
<br />
100<br />
<br />
<br />
<br />
50<br />
<br />
staurospor<strong>in</strong>e<br />
<br />
H-89<br />
Ro-318220<br />
0<br />
KT5720<br />
<br />
-8 -7 -6 -5 -9 -4<br />
<br />
<br />
log [drug] (M)<br />
<br />
Test<strong>in</strong>g<br />
conditions<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
For further details and updated <strong>in</strong>formation on assays:<br />
❚ Please go to www.cerep.com catalog onl<strong>in</strong>e or contact us at sales@cerep.com<br />
-10 -9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4<br />
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – Ch<strong>in</strong>a: +86 21 5132 0568<br />
Assay developed <strong>in</strong> 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®<br />
Human Q Standard turnaround time<br />
Assay list<br />
& <strong>in</strong>dex
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