in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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131<br />
CaMK1d<br />
Ref. 2922<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<br />
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 : 3.3 nM)<br />
Corcoran, E.E. et al. (2003) J. Biol. Chem., 12: 10516-10522.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [CaMK] ❚<br />
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<br />
<br />
<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
CaMK2a<br />
Ref. 3024<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
BioPr<strong>in</strong>t ® profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-CGSGSGRPRTSSFAEG<br />
(50 nM)<br />
Measured product phospho-Ulight-CGSGSGRPRTSSFAEG<br />
Detection method LANCE<br />
Reference<br />
AIP (IC 50 : 88 nM)<br />
Ichida, A. and Fujisawa, H. (1995) J. Biol. Chem., 270: 2163-2170.<br />
enzyme activity (% of control)<br />
<br />
100 <br />
<br />
<br />
50<br />
<br />
AIP<br />
<br />
staurospor<strong>in</strong>e<br />
K252a<br />
0<br />
Ro-318220<br />
<br />
-9 -8 -7 -6 -10 -5<br />
<br />
<br />
log [drug] (M)<br />
<br />
Ion<br />
channels<br />
Transporters<br />
CaMK2g<br />
Ref. 2740<br />
Q 3 weeks<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 : 0.84 nM)<br />
Ishida, A. and Fujisawa, H. (1995) J. Biol. Chem., 270: 2163-2170.<br />
<br />
<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
-11 -10 -9 -8 -7 -6 -5 -4 -3<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
-12<br />
-10 -9 -8 -7 -6<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
<br />
-12 -11 -10 -8 -7 -6 -9 -5 -4 -3<br />
<br />
-10 -9 -8 -7 -6 -12 -11 -5<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
CaMK4<br />
Ref. 1582<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 (E. coli)<br />
Substrate ATP + biot<strong>in</strong>yl-long CREB derived peptide<br />
(100 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-long CREB derived peptide<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 50 nM)<br />
Enslen, H. et al. (1994) J. Biol. Chem., 269: 15520-15527.<br />
enzyme activity (% of control)<br />
<br />
100 <br />
<br />
<br />
50<br />
<br />
<br />
staurospor<strong>in</strong>e<br />
K252a<br />
0<br />
AIP<br />
<br />
-8 -7 -6 -5 -9 -4<br />
<br />
<br />
log [drug] (M)<br />
<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
CHK1<br />
Ref. 2917<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 (<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 : 5.6 nM)<br />
Zhao, B. et. al. (2002) J. Biol. Chem., 277: 46609-46615.<br />
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<br />
<br />
<br />
<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
CHK2<br />
Ref. 2882<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 (<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 : 27 nM)<br />
Ng, C.-P. et. al. (2004) J. Biol. Chem., 279: 8808-8819.<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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