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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 />

<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

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