in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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135<br />
PhKg1<br />
Ref. 2745<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 + 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 : 0.78 nM)<br />
Burw<strong>in</strong>kel, B. et al. (2003) Eur. J. Hum. Genet., 11: 516-526.<br />
prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [CaMK] ❚<br />
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<strong>Cerep</strong><br />
services<br />
Receptors<br />
PhKg2<br />
Ref. 2622<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 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 : 4.6 nM)<br />
Burw<strong>in</strong>kel, B. et al. (1998) Hum. Mol. Gen., 7: 149-154.<br />
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Ion<br />
channels<br />
Transporters<br />
Pim1 k<strong>in</strong>ase<br />
Ref. 2919<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 + 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 : 35 nM)<br />
Hoover, D. et. al. (1991) J. Biol. Chem., 266: 14018-14023.<br />
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K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
Pim2 k<strong>in</strong>ase<br />
Ref. 2920<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 (<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 : 17 nM)<br />
Van der Lugt, N.M. et. al. (1995) Embo. J., 14: 2536-2544.<br />
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Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
PKD1 (PKCµ)<br />
Ref. 2204<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (Sf21 cells)<br />
Substrate ATP + biot<strong>in</strong>yl-bAbAbAKEAKEKRQEQIAKRR<br />
RLSSLRASTSKSGGSQK (20 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKEAKEKRQEQIAK<br />
RRRLSSLRASTSKSGGSQK<br />
Detection method HTRF<br />
Reference<br />
Ro-318220 (IC 50 : 8 nM)<br />
Hausser, A. et al. (1999) J. Biol. Chem., 274: 9258-9264.<br />
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Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
PKD2<br />
Ref. 1729<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-bAbAbAKKKVSRSGLYRSPSM<br />
PENLNRPR (25 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAKKKVSRSGLYRSP<br />
SMPENLNRPR<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 8.7 nM)<br />
Sturany, S. et al. (2001) J. Biol. Chem., 276: 3310-3318.<br />
enzyme activity (% of control)<br />
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100<br />
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50<br />
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staurospor<strong>in</strong>e<br />
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H-89<br />
Ro-318220<br />
0<br />
K252a<br />
-10 -9 -8 -7 -6 -5 -4<br />
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log [drug] (M)<br />
-10 -9 -8 -7 -6 -5 -4<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex<br />
-10 -9 -8 -7 -6 -5 -4<br />
-8 -7 -6 -5 -4