in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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159<br />
HDACs ❚<br />
HDAC3<br />
Ref. 2083<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
Diversity profile<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
fluorogenic HDAC substrate (50 µM)<br />
Measured product fluoro-lys<strong>in</strong>e<br />
Detection method fluorimetry<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 5 nM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
trichostat<strong>in</strong> A<br />
scriptaid<br />
sodium butyrate<br />
α-compound 8<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
HDAC4<br />
Ref. 2493<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
Diversity profile<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
fluorogenic HDAC substrate class 2a<br />
(20 µM)<br />
Measured product fluoro-lys<strong>in</strong>e<br />
Detection method fluorimetry<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 3.3 µM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
<br />
-10 -9 -8 -7 -6<br />
-10 -7 -9 -8 -6 -5 -4<br />
<br />
<br />
-12 -11 -6 -5<br />
-10 -9 -8 -7<br />
<br />
<br />
<br />
<br />
α<br />
Ion<br />
channels<br />
Transporters<br />
HDAC5<br />
Ref. 2494<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
fluorogenic HDAC substrate class 2a (20 µM)<br />
Measured product fluoro-lys<strong>in</strong>e<br />
Detection method fluorimetry<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 1.3 µM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
α<br />
K<strong>in</strong>ases<br />
<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
HDAC6<br />
Ref. 2495<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
Diversity profile<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
fluorogenic HDAC substrate (25 µM)<br />
Measured product fluoro-lys<strong>in</strong>e<br />
Detection method fluorimetry<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 30 nM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
α<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
HDAC7<br />
Source<br />
Substrate<br />
Measured product<br />
Detection method<br />
human recomb<strong>in</strong>ant<br />
fluorogenic HDAC substrate class 2a<br />
(50 µM)<br />
fluoro-lys<strong>in</strong>e<br />
fluorimetry<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
α<br />
<br />
Standard<br />
profiles<br />
Ref. 2610<br />
Q 3 weeks<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 2.1 µM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
<br />
<br />
<br />
<br />
Test<strong>in</strong>g<br />
conditions<br />
HDAC8<br />
Ref. 2247<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
fluorogenic HDAC substrate (400 µM)<br />
Measured product fluoro-lys<strong>in</strong>e<br />
Detection method fluorimetry<br />
Reference<br />
trichostat<strong>in</strong> A (IC 50 : 400 nM)<br />
Strahl, B.D. and Allis, C.D. (2000) Nature, 403: 41-45.<br />
enzyme activity (% of control)<br />
<br />
100 <br />
<br />
<br />
<br />
50<br />
<br />
trichostat<strong>in</strong> A<br />
<br />
sriptaid<br />
sodium butyrate<br />
0<br />
α-compound 8<br />
-10 -9 -8 -7 -6 -5 -4<br />
-11<br />
<br />
<br />
log [drug] (M)<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 -3
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