in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
Create successful ePaper yourself
Turn your PDF publications into a flip-book with our unique Google optimized e-Paper software.
119<br />
prote<strong>in</strong>-tyros<strong>in</strong>e k<strong>in</strong>ases [Ctk] ❚<br />
Brk<br />
Ref. 3063<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<br />
ATP + Ulight-TK peptide<br />
(100 nM)<br />
Measured product phospho-Ulight-TK peptide<br />
Detection method LANCE<br />
Reference<br />
PP1 (IC 50 : 35 nM)<br />
Qiu, H. and Miller, W.T. (2002) J. Biol. Chem., 277: 34634-34641.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
BTK<br />
Ref. 1589<br />
Q 3 weeks<br />
CSK<br />
Ref. 1524<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + biot<strong>in</strong>yl-bAbAbAEEEPQYEEIPIYLELLP<br />
(1.8 µM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAEEEPQYEEIPIYLELLP<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 50 nM)<br />
Mahajan, S. et al. (2001) J. Biol. Chem., 276: 31216-31228.<br />
-9 -8 -7 -6 -5 -4<br />
Source<br />
human recomb<strong>in</strong>ant (E. coli)<br />
Substrate<br />
ATP + biot<strong>in</strong>yl-bAbAbAEEEPQYEEIPIYLELLP<br />
(40 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAEEEPQYEEIPIYLELLP<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 96 nM)<br />
Ruzzene, M. et al. (1997) Eur. J. Biochem., 246: 433-439.<br />
enzyme activity (% of control)<br />
enzyme activity (% of control)<br />
<br />
<br />
100<br />
<br />
50<br />
<br />
staurospor<strong>in</strong>e<br />
PP1<br />
AG538<br />
0<br />
AG1112 <br />
-8 -7 -5 -10 -9 -6 -4<br />
<br />
<br />
log [drug] (M)<br />
<br />
-8 -7 -6 -5 -4<br />
-9<br />
100<br />
-9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4<br />
50<br />
-10 -9 -8 -7 -6 -5 -4<br />
staurospor<strong>in</strong>e<br />
PP1<br />
PP2<br />
0<br />
AG1112<br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
Ion<br />
channels<br />
Transporters<br />
<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
CTK<br />
Ref. 2638<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<br />
ATP + Ulight-Poly GAT[EAY(1:1:1)]n<br />
(5 nM)<br />
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 593 nM)<br />
Wood, A. et al. (2007) Mol. Cell. Biol., 27: 709-720.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
FAK<br />
Ref. 3065<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 (Sf9 cells)<br />
Substrate<br />
ATP + Ulight-TK peptide<br />
(100 nM)<br />
Measured product phospho-Ulight-TK peptide<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 27 nM)<br />
McLean, G.W. et al. (2000) J. Biol. Chem., 275: 23333-23339.<br />
<br />
<br />
<br />
<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 />
Fer k<strong>in</strong>ase<br />
Ref. 2641<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<br />
ATP + Ulight-Poly GAT[EAY(1:1:1)]n<br />
(5 nM)<br />
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 4.1 nM)<br />
Kim, L. and Wong T.W. (1998) J. Biol. Chem., 273: 23542-23548.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
Change language