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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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<br />

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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<br />

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 />

<br />

100<br />

<br />

50<br />

<br />

staurospor<strong>in</strong>e<br />

<br />

H-89<br />

Ro-318220<br />

0<br />

K252a<br />

-10 -9 -8 -7 -6 -5 -4<br />

<br />

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

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