in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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118 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ Prote<strong>in</strong>-tyros<strong>in</strong>e k<strong>in</strong>ases [CTK]<br />
Abl k<strong>in</strong>ase<br />
Ref. 3056<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 />
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<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 : 101 nM)<br />
Park, Y.M. et al. (1999) Anal. Biochem., 269: 94-104.<br />
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Ack<br />
Ref. 3052<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-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 : 2.6 nM)<br />
Mahajan, N.P. et al. (2005) Cancer. Res., 65: 10514-10523.<br />
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Arg k<strong>in</strong>ase<br />
Ref. 3057<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-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 : 60.8 nM)<br />
De Keersmaecker, K. and Cools, J. (2006) Leukemia, 20: 200-205.<br />
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BLK<br />
Ref. 1697<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + biot<strong>in</strong>yl-bAbAbAAEEEIYEEIEAKKK<br />
(300 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAAEEEIYEEIEAKKK<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 5.4 nM)<br />
Saouaf, S.J. et al. (1995) J. Biol. Chem., 270: 27072-27078.<br />
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BMX (Etk) k<strong>in</strong>ase<br />
Ref. 1587<br />
Q 3 weeks<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 />
(400 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 : 93 nM)<br />
Jiang, T. et al. (2004) J. Biol.Chem., 279: 50181-50189.<br />
enzyme activity (% of control)<br />
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100<br />
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50<br />
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0<br />
-10 -9 -8 -7 -6 -5 -4<br />
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log [drug] (M)<br />
staurospor<strong>in</strong>e<br />
PP1<br />
AG538<br />
AG1112<br />
For further details and updated <strong>in</strong>formation on assays:<br />
❚ Please go to www.cerep.com catalog onl<strong>in</strong>e or contact us at sales@cerep.com<br />
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – Ch<strong>in</strong>a: +86 21 5132 0568<br />
Assay developed <strong>in</strong> 2010 New assay conditions and/or assay converted from HTRF ® to LANCEUltra ®<br />
Human Q Standard turnaround time
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