Inhibitor | K252a  

Compound name Brutto MW CAS PubChem CID Action Reference Reference
K252a   C27H21N3O5 467.50 99533-80-9 127357 CaMKII Cools J. (2004) Cancer Res. 64 6385 Chin L.S. (1999) Cancer Invest. 17 391

Screening Results Chart

Screening Results Tables

Screen Conc: 0.10µM
Kinase % Activity Remaining Standard Deviation
AMPK 17 7
BRSK2
9
0
BTK
8
2
CAMK1 46 10
CAMKK beta 57 1
CDK2-Cyclin A 41 3
CHK1
1
0
CHK2 14 20
CK1 delta 86 1
CK2 99 3
CSK 84 10
DYRK1A 26 0
DYRK2 26 4
DYRK3
7
1
EF2K 102 10
EPH-A2 97 9
EPH-B3 112 8
ERK1 24 3
ERK2 44 6
ERK8
3
0
FGF-R1 50 0
GSK3 beta 66 5
HIPK2 59 6
IGF-1R 49 8
IKK beta 54 11
IKK epsilon 19 0
IR 94 6
IRR 29 1
JNK1 65 12
JNK2 59 2
Lck 43 1
MAPKAP-K2
4
1
MARK3
8
0
MELK
5
1
MKK1
1
0
MNK1 28 1
MNK2
6
0
MSK1 28 7
MST2
4
2
MST4 244 41
NEK2a 99 7
NEK6 93 4
p38 alpha MAPK 86 10
p38 beta MAPK 110 22
p38 delta MAPK 86 2
p38 gamma MAPK 60 7
PAK4 21 0
PAK5 29 0
PAK6 30 2
PDK1
7
2
PHK
0
0
PIM1 18 0
PIM2 51 11
PIM3
3
0
PKA 51 7
PKB alpha 82 4
PKB beta 78 3
PKC alpha 86 2
PKC zeta 77 17
PKD1
4
3
PLK1 72 8
PRAK 85 6
PRK2
7
0
ROCK 2 68 6
RSK1
6
0
RSK2 28 8
S6K1 28 2
SGK1 14 0
SmMLCK 32 2
Src 53 3
SRPK1 92 2
SYK 12 0
TBK1 12 6
VEGFR1
8
1
YES1 49 9
Screen Conc: 1.00µM
Kinase % Activity Remaining Standard Deviation
AMPK
4
2
Aurora A
0
0
Aurora B
5
2
BRSK1 11 2
BRSK2
3
0
BTK
4
1
CAMK1 15 6
CAMKK beta 18 4
CDK2-Cyclin A
1
0
CHK1
9
2
CHK2
4
0
CK1 delta 90 5
CK2 81 9
CLK2
2
0
CSK 22 2
DAPK1
6
2
DYRK1A
1
1
DYRK2
1
0
DYRK3
1
0
EF2K 100 5
EPH-A2 29 6
EPH-A4 19 1
EPH-B2 44 3
EPH-B3 16 0
EPH-B4 75 13
ERK1
8
1
ERK2
3
1
ERK8
1
0
FGF-R1
6
0
GCK
4
2
GSK3 beta 15 0
HER4 14 3
HIPK1 34 4
HIPK2
4
1
HIPK3 24 0
IGF-1R
3
1
IKK beta
9
0
IKK epsilon
2
1
IR
5
0
IRAK4
2
1
IRR 19 2
JAK2
1
1
JNK1
3
1
JNK2
5
0
JNK3
3
0
Lck
6
3
LKB1 11 1
MAPKAP-K2
2
1
MAPKAP-K3 49 1
MARK1
6
1
MARK2 24 9
MARK3
5
1
MARK4
7
1
MEKK1
2
1
MELK
5
3
MINK1
3
1
MKK1
0
1
MLK1 43 52
MLK3
3
0
MNK1 41 5
MNK2
8
4
MSK1
4
0
MST2
2
0
MST4
9
1
NEK2a 48 3
NEK6 96 2
NUAK1
7
0
p38 alpha MAPK 91 6
p38 beta MAPK 42 0
p38 delta MAPK 41 1
p38 gamma MAPK
8
0
PAK2 11 2
PAK4
6
1
PAK5
5
0
PAK6
8
1
PDK1
3
3
PHK
1
0
PIM1
2
0
PIM2 12 1
PIM3
5
1
PKA
3
0
PKB alpha 19 2
PKB beta 37 12
PKC alpha
5
1
PKC zeta 17 4
PKD1 15 2
PLK1 41 1
PRAK 14 2
PRK2
6
1
RIPK2
4
0
ROCK 2 12 2
RSK1
1
1
RSK2
1
0
S6K1
9
0
SGK1
8
1
SmMLCK
4
1
Src
6
1
SRPK1 54 4
SYK
5
3
TAK1
4
1
TBK1
3
1
TrkA
6
1
TTK 18 2
VEGFR1
6
1
YES1
10
0
Screen Conc: 10.00µM
Kinase % Activity Remaining Standard Deviation
ABL 32 2
AMPK 14 1
ASK1
6
0
Aurora A
0
0
Aurora B 35 3
BRK
4
3
BRSK1
5
3
BRSK2
3
1
BTK 19 4
CAMK1
3
1
CAMKK beta
5
1
CDK2-Cyclin A
6
1
CHK1
7
0
CHK2
5
8
CK1 delta 63 23
CK2 72 1
CLK2
3
0
CSK 28 7
DAPK1
8
0
DYRK1A
0
0
DYRK2
5
6
DYRK3
4
1
EF2K 105 1
EIF2AK3 15 1
EPH-A2
8
1
EPH-A4
7
0
EPH-B1 19 1
EPH-B2
8
1
EPH-B3 49 0
EPH-B4 22 1
ERK1 14 5
ERK2
2
1
ERK8
9
1
FGF-R1
3
1
GCK
3
0
GSK3 beta
2
1
HER4 13 0
HIPK1
7
0
HIPK2
2
0
HIPK3
4
0
IGF-1R
0
0
IKK beta
4
1
IKK epsilon
2
0
IR
1
0
IRAK1
2
1
IRAK4
3
1
IRR
2
1
JAK2
3
3
JNK1
1
0
JNK2
2
0
JNK3
5
0
Lck
10
2
LKB1 11 1
MAPKAP-K2
0
0
MAPKAP-K3 11 3
MARK1 16 1
MARK2 20 14
MARK3
1
0
MARK4
9
0
MEKK1 54 5
MELK
9
4
MINK1 24 1
MKK1
1
0
MKK2
5
1
MKK6 32 6
MLK1 15 3
MLK3 11 0
MNK1 42 1
MNK2 39 2
MPSK1 12 1
MSK1
1
0
MST2 14 4
MST4 14 1
NEK2a 20 5
NEK6 85 0
NUAK1
2
0
OSR1
4
0
p38 alpha MAPK 49 6
p38 beta MAPK 24 2
p38 delta MAPK 11 0
p38 gamma MAPK
7
3
PAK2
4
0
PAK4
3
1
PAK5
4
1
PAK6
1
0
PDK1
5
0
PHK
5
2
PIM1
5
0
PIM2
2
0
PIM3
2
0
PKA
2
0
PKB alpha
5
1
PKB beta 18 0
PKC alpha 18 4
PKC gamma 28 3
PKC zeta
3
1
PKD1
8
5
PLK1 31 6
PRAK
7
1
PRK2
4
0
RIPK2 14 4
ROCK 2 21 6
RSK1
3
0
RSK2
1
1
S6K1
3
0
SGK1
8
3
SmMLCK 12 2
Src
4
1
SRPK1 16 1
STK33
6
0
SYK
5
1
TAK1
3
3
TAO1
5
1
TBK1 11 9
TIE2
7
1
TLK1
3
2
TrkA
2
1
TTK 19 1
VEGFR1
2
1
YES1
6
3
ZAP70
6
1