in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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141<br />
PKCe<br />
Ref. 2044<br />
Q 3 weeks<br />
PKCz<br />
Ref. 2045<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-bAbAbAKIQASFRGHMARKK<br />
(400 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKIQASFRGHMA<br />
RKK<br />
Detection method HTRF<br />
Reference<br />
Bis 10 (IC 50 : 8 nM)<br />
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate ATP + biot<strong>in</strong>yl-βAβAβAKIQASFRGHMARKK<br />
(600 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-βAβAβAKIQASFRGHMARKK<br />
Detection method HTRF<br />
Reference<br />
Bis 10 (IC 50 : 61.3 nM)<br />
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [AGC] ❚<br />
enzyme activity (% of control)<br />
<br />
100<br />
50<br />
0<br />
<br />
<br />
<br />
-11 -10 -9 -8 -7 -6<br />
log [drug] (M)<br />
-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 />
-10 -9 -8 -7 -6 -5 -4<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5<br />
<br />
Bis 10<br />
staurospor<strong>in</strong>e<br />
Ro-318220<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
Ion<br />
channels<br />
Transporters<br />
PKCh<br />
Ref. 2046<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-βAβAβAKIQASFRGHMARKK<br />
(200 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-βAβAβAKIQASFRGHMARKK<br />
Detection method HTRF<br />
Reference<br />
Bis 10 (IC 50 : 53.6 nM)<br />
Chen, S.J. et al. (1993) Biochemistry, 32: 1032-1039.<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 />
PKCq<br />
Ref. 2120<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-βAβAβAKIQASFRGHMARKK<br />
(200 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-βAβAβAKIQASFRGHMARKK<br />
Detection method HTRF<br />
Reference<br />
Bis 10 (IC 50 : 1.55 nM)<br />
Manicassamy, S. et al. (2006) Cell. Mol. Immun., 3: 263-270.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
PKCi<br />
Ref. 2121<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-βAβAβAKIQASFRGHMARKK<br />
(200 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-βAβAβAKIQASFRGHMARKK<br />
Detection method HTRF<br />
Reference<br />
Bis 10 (IC 50 : 100 nM)<br />
Stall<strong>in</strong>gs-Mann, M. et al. (2006) Cancer Res., 66: 1767-1774.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
PKG1a<br />
Ref. 2469<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 (Sf21 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 : 11.2 nM)<br />
Hou, Y. et al. (2003) J. Biol. Chem., 278: 16706-16712.<br />
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<br />
<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex