in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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144 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [AGC]<br />
SGK2<br />
Ref. 1969<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate ATP + biot<strong>in</strong>yl-bAbAbAKGSGSGRPRTSSFAEF<br />
(20 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKGSGSGRPRTSSFAEF<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 270 nM)<br />
Kobayashi, T. et al. (1999) Biochem. J., 344: 189-197.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
staurospor<strong>in</strong>e<br />
SP600125<br />
H-89<br />
Ro-318220<br />
SGK3<br />
Ref. 2790<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 : 123.5 nM)<br />
Kobayashi, T. et al. (1999) Biochem. J., 344: 189-197.<br />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
<br />
-8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5<br />
-9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5<br />
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<br />
❚ prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [CK1]<br />
<br />
<br />
CK1a<br />
Ref. 1716<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-ARTKQTARKSTGGKAPRKQLAG<br />
CG (25 nM)<br />
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />
AGCG<br />
Detection method LANCE<br />
Reference<br />
hymenialdis<strong>in</strong> (IC 50 : 5.25 µM)<br />
Pulgar, V. et al. (1996) Biochem. J., 242: 519-528.<br />
<br />
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<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
CK1e<br />
Ref. 2630<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAG<br />
CG (25 nM)<br />
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />
AGCG<br />
Detection method LANCE<br />
Reference<br />
hymenialdis<strong>in</strong> (IC 50 : 3 µM)<br />
Brockschmidt, C. et al. (2008) Gut., 57: 799-806.<br />
<br />
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<br />
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❚ prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [STE]<br />
<br />
<br />
<br />
ASK1<br />
Ref. 2124<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 + biot<strong>in</strong>yl-bAbAbAGISALQDGLKRREILSR<br />
PPSYRKLL (1.4 µM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAGISALQDGLKRREI<br />
LSRPPSYRKLL<br />
Detection method HTRF<br />
Reference staurospor<strong>in</strong>e (IC 50 : 8 nM)<br />
Sayama, K. et al. (2001) J. Biol. Chem., 276: 999-1004.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
<br />
<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
staurospor<strong>in</strong>e<br />
Ro-318220<br />
H-89<br />
K252a<br />
-10 -9 -8 -7 -6 -5 -4 -3
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