in vitro PHARMACOLOGY 2011 CATALOG - Cerep

128 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [CMGC]
GSK3b
cellul ar
Ref. 3102
Ref. 3107
Q 3 weeks
Activator effect
Inhibitor effect
Source
A431 cells
Measured product phosphorylation
Detection method AlphaScreen
Activator effect Control EGF (100 nM)
Reference EGF (EC 50 : 0.083 nM)
Inhibitor effect Stimulant EGF (0.1 nM)
Reference AG1478 (IC 50 : 75 nM)
[Solvent] must be kept 0.1%
HIPK2
Ref. 2915
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(50 nM)
Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
Detection method LANCE
Reference
staurosporine (IC 50 : 500 nM)
Di Stefano, V. et al. (2004) Exp. Cell. Res., 293: 311-320.
HIPK3
Ref. 1980
Q 3 weeks
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-MBP
(400 nM)
Measured product phospho-biotinyl-MBP
Detection method HTRF
Reference
staurosporine (IC 50 : 250 nM)
Rochat-Steiner, V. et al. (2000) J. Exp. Med., 192: 1165-1174.
enzyme activity (% of control)
100
50
staurosporine
Ro-318220
0
K252a
-8 -7 -6 -9 -5
log [drug] (M)
HIPK4
Ref. 1981
Q 3 weeks
Source
Substrate
Measured product
Detection method
Reference
-11 -10 -9 -8 -7 -6 -5 -4 -3
human recombinant (insect cells)
ATP + biotinyl-MBP
(200 nM)
phospho-biotinyl-MBP
HTRF
-10
staurosporine (IC 50 : 250 nM)
Di Stefano, V. et al. (2004) Exp. Cell. Res., 293: 311-320.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100-10
-9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
50
-10 -9 -8 -7 -6 -5
staurosporine
H-89
Ro-318220
0
K252a
-9 -8 -7 -6 -5 -4 -3
log [drug] (M)
JNK1
Ref. 2880
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Comprehensive kinase profile
Source
Substrate
Measured product
Detection method
Reference
human recombinant (E.coli)
-11 -10 -9 -8 -7 -6 -5 -4 -3
-10
-9 -8 -7 -6 -5 -4
ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide
(100 nM)
phospho-Ulight-CFFKNIVTPRTPPPSQGKamide
LANCE
staurosporine (IC 50 : 1550 nM)
Bennett, B.L. et al. (2001) Proc. Natl. Acad. Sci. USA., 98: 13681-13686.
-10 -9 -8 -7 -6 -5 -4 -3
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-10 -9 -8 -7 -6 -5
JNK2
Ref. 3368
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (E. Coli)
Substrate
ATP + ATF-2
(75 nM)
Measured product phospho-ATF-2
Detection method LANCE
Reference
SP600125 (IC 50 : 69.9 nM)
Bennett, B.L. et al. (2001) Proc. Natl. Acad. Sci. USA, 98: 13681-13686.