in vitro PHARMACOLOGY 2011 CATALOG - Cerep

142 in vitro pharmacology 2011 catalog
❚ protein-SERINE/THREONINE kinases [AGC]
PKG1b
Ref. 1730
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate ATP + biotinyl-KEAKEKRQEQIAKRRRLSSLRA
STSKSGGSQK (20 nM)
Measured product phospho-biotinyl-KEAKEKRQEQIAKRRRLSSL
RASTSKSGGSQK
Detection method HTRF
Reference
staurosporine (IC 50 : 26.8 nM)
Orstavik, S. et al. (1997), Genomics, 42: 311-318.
enzyme activity (% of control)
100
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
staurosporine
H-89
Ro-318220
K252a
PKG2
Ref. 1928
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate ATP + biotinyl-KEAKEKRQEQIAKRRRLSSLRA
STSKSGGSQK (50 nM)
Measured product phospho-biotinyl-KEAKEKRQEQIAKRRRLSSL
RASTSKSGGSQK
Detection method HTRF
Reference
staurosporine (IC 50 : 1.1 nM)
Ross, H. et aL. (2002) Biochem. J., 366: 977-981.
enzyme activity (% of control)
-11 -10 -9 -8 -7 -6 -5 -4
100
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-8 -7 -6 -9 -5 -4
50
staurosporine
H-89
Ro-318220
0
K252a
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
PKN1
Ref. 2615
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 2 nM)
Lartey, J. et al. (2007) Biol. Reprod., 76: 971-982.
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5 -4
PKN2
Ref. 2746
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + CREBtide (CKRREILSRRPSYRK)
(25 nM)
Measured product phospho-CREBtide (CKRREILSRRPSYRK)
Detection method LANCE
Reference
staurosporine (IC 50 : 1.23 nM)
Schmidt, A. et al. (2007) Embo. J., 26: 1624-1636.
PRKX
Ref. 2681
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 6.8 nM)
Chiorini, J.A. et al. (1998) Mol. Cell. Biol., 18: 5921-5929.
ROCK1
Ref. 3364
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate ATP + Ulight-RRRSLLE
(50 nM)
Measured product phospho-Ulight-RRRSLLE
Detection method LANCE
Reference
staurosporine (IC 50 : 20.2 nM)
Doe, C. et al.(2007) J. Pharmacol. Exp. Ther., 320: 89-98.