in vitro PHARMACOLOGY 2011 CATALOG - Cerep

146 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [STE]
MEKK3 (MAP3K3)
Ref. 2760
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 6.2 nM)
Samanta, A.K. et al. (2004) J. Biol. Chem., 279: 7576-7583.
MEKK4 (MAP3K4)
Ref. 2759
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG
(25 nM)
Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL
AGCG
Detection method LANCE
Reference staurosporine (IC 50 : 110 nM)
Chi, H. et al. (2005) Proc. Natl. Acad. Sci. USA, 102: 3846-3851.
MINK
Ref. 2113
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-bAbAbAAAARARTSSFAEPG
(200 nM)
Measured product phospho-biotinyl-bAbAbAAAARARTSSFAEPG
Detection method HTRF
Reference
Bis 10 (IC 50 : 27 nM)
Nicke, B. et al. (2005) Mol. Cell., 20: 673-685.
enzyme activity (% of control)
100
50
0
Bis 10
staurosporine
H-89
SB202190
-8 -7 -5 -4
-10 -9 -6
log [drug] (M)
MKK4/JNK1
Ref. 1927
Q 3 weeks
Included in:
Organ safety profile
Source
mouse recombinant (E. coli)
Substrate ATP + inactive JNK1
(0.19 µg/ml)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 36 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6
-10 -7 -9 -8 -6 -5 -4
-12 -11 -10 -7 -6 -5
-9 -8
MKK4/JNK2
Ref. 1953
Q 3 weeks
Source
mouse recombinant
Substrate ATP + inactive JNK2 (MAPK9)
(0.05 µg/mL)
Measured product phospho-ATF-2
Detection method HTRF
Reference
staurosporine (IC 50 : 41 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
enzyme activity (% of control)
100
50
staurosporine
SP600125
0
SB202190
-9 -8 -7 -6 -5 -4
log [drug] (M)
MKK6
Ref. 2931
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + inactive p38a
(50 nM)
Measured product phospho-p38a
Detection method LANCE
Reference
-11
-10 -9 -8 -7 -6 -5 -4
-10
staurosporine (IC 50 : 11 nM)
Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891.
-9 -8 -7 -6 -5 -4
-3
-10
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5 -4
-3