in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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133<br />
MAPKAPK2<br />
Ref. 3367<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 (E. coli)<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 : 453 nM)<br />
Tan, Y. et al. (1996) Embo. J., 15: 4629-4642.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [CaMK] ❚<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
MAPKAPK5 (PRAK)<br />
Ref. 2684<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 + 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 : 2047 nM)<br />
Ross, H. et. al. (2002) Biochem. J., 366: 977-981.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Ion<br />
channels<br />
Transporters<br />
MARK1<br />
Ref. 3362<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<br />
Substrate ATP + Ulight-RRRSLLE<br />
(50 nM)<br />
Measured product phospho-Ulight-RRRSLLE<br />
Detection method LANCE<br />
Reference staurospor<strong>in</strong>e (IC 50 :14.4 nM)<br />
Timm, T. et al. (2008) BMC Neurosc., 9: S9.<br />
<br />
<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 />
MARK2<br />
Ref. 1966<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-bAbAbAKKKVSRSGLYRSPMP<br />
ENLNRPR (80 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKKKVSRSGLYRSP<br />
MPENLNRPR<br />
Detection method HTRF<br />
Reference<br />
H-89 (IC 50 : 3.067 µM)<br />
Biernat, J. et al. (2002) Mol. Biol. Cell., 13: 4013-4028.<br />
enzyme activity (% of control)<br />
100<br />
<br />
<br />
50<br />
H-89<br />
Ro-318220<br />
0<br />
K252a<br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
MARK3<br />
Ref. 2789<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 : 7.46 nM)<br />
Goransson, O. et al. (2006) J. Cell Sci., 119: 4059-4070.<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
MARK4<br />
Ref. 1967<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-bAbAbAKKKVSRSGLYRSPMP<br />
ENLNRPR (80 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKKKVSRSGLYRSP<br />
MMPENLNRPR<br />
Detection method HTRF<br />
Reference<br />
hymenialdis<strong>in</strong>e (IC 50 : 80 nM)<br />
Schneider, A. et al. (2004) J. Neurochem., 88: 1114-1126.<br />
enzyme activity (% of control)<br />
<br />
100<br />
<br />
<br />
<br />
50<br />
<br />
hymenialdis<strong>in</strong>e<br />
<br />
staurospor<strong>in</strong>e<br />
H-89<br />
0<br />
K252a<br />
<br />
-9 -8 -7 -6 -5 -4<br />
-10<br />
<br />
log [drug] (M)<br />
<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex<br />
-10 -9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4