in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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143<br />
ROCK2<br />
Ref. 2884<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-RRRSLLE<br />
(100 nM)<br />
Measured product phospho-Ulight-RRRSLLE<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 13 nM)<br />
Turner, M.S. et al. (2002) Arch. Biochem. Biophys., 405: 13-20.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [AGC] ❚<br />
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<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
RSK1<br />
Ref. 2616<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 + CREBtide (CKRREILSRRPSYRK)<br />
(25 nM)<br />
Measured product phospho-CREBtide (CKRREILSRRPSYRK)<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 1.9 nM)<br />
Roberts, N.A. et al. (2005) Brit. J. Pharmacol., 145: 477-489.<br />
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Ion<br />
channels<br />
Transporters<br />
RSK2<br />
Ref. 2928<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 (<strong>in</strong>sect cells)<br />
Substrate ATP + CREBtide (CKRREILSRRPSYRK)<br />
(25 nM)<br />
Measured product phospho-CREBtide (CKRREILSRRPSYRK)<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 2.63 nM)<br />
Cho, Y.Y. et al. (2007) Cancer Res., 67: 8104-8112.<br />
enzyme activity (% of control)<br />
<br />
100<br />
<br />
<br />
<br />
50<br />
<br />
staurospor<strong>in</strong>e<br />
Gö 6850<br />
kaempferol<br />
0<br />
SL0101<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3<br />
<br />
log [drug] (M)<br />
<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
RSK3<br />
Ref. 2682<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-RRRSLLE<br />
(50 nM)<br />
Measured product phospho-Ulight-RRRSLLE<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 5 nM)<br />
Chen, R.H. et al. (1992) Mol. Cell. Biol., 12: 915-927.<br />
<br />
<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
-11 -10 -9 -8 -7 -6 -5 -4 -3<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6<br />
<br />
<br />
-10 -7 -4<br />
-9 -8 -6 -5<br />
<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3<br />
<br />
-10 -9 -8 -7 -6 -5<br />
-12 -11<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
SGK1<br />
Ref. 2929<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-RRRSLLE<br />
(50 nM)<br />
Measured product phospho-Ulight-RRRSLLE<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 12 nM)<br />
Ross, H. et al. (2002) Biochem. J., 366: 977-981.<br />
<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
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Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
<br />
❚ Assays converted from HTRF ® to LANCEUltra ® technology<br />
<br />
A majority of our k<strong>in</strong>ase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET with the<br />
difference <strong>in</strong> europium labell<strong>in</strong>g: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® .<br />
<br />
Assays are converted follow<strong>in</strong>g a standard procedure consist<strong>in</strong>g of time course experiment, Km determ<strong>in</strong>ation and pharmacology<br />
characterization of the enzyme by <strong>in</strong>hibit<strong>in</strong>g its activity with known <strong>in</strong>hibitors. IC 50 values obta<strong>in</strong>ed for known <strong>in</strong>hibitors are compared<br />
<br />
to literature and to those obta<strong>in</strong>ed us<strong>in</strong>g HTRF ® technology. If all values are <strong>in</strong> agreement with the previous ones, LANCE ® technology is<br />
validated for the k<strong>in</strong>ase of <strong>in</strong>terest.<br />
<br />
This conversion allows us to standardize and automate our k<strong>in</strong>ase assays provid<strong>in</strong>g shorter turnaround times for both profil<strong>in</strong>g and screen<strong>in</strong>g<br />
experiments.<br />
<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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