|
Target
|
Inhibitor
|
IC50 (M)
|
Acridine orange 45 min.
|
Acridine orange Quenching
|
Influx - % Inh. at 10 μM
|
Influx Quenching
|
Resorption - % Inh at 10 μM
|
Alamar - % Inh. at 10 μM
|
|---|
|
PDGFRK
|
AG-370
|
20
|
No
|
No
|
20
|
Yes
|
0
|
0
|
| |
AG-1296
|
1
|
No
|
No
|
15
|
Yes
|
0
|
0
|
|
EGFRK/PDGFRK
|
AG-494
|
1.2
|
No
|
No
|
55
|
No
|
0
|
0
|
| |
Tyrphostin 46
|
9.2
|
No
|
No
|
0
|
No
|
0
|
0
|
|
EGFRK
|
Lavendustin A
|
0.011
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
RG-14620
|
3
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
Tyrphostin 23
|
35
|
No
|
No
|
45
|
Yes
|
0
|
0
|
| |
Tyrphostin 25
|
3
|
No
|
No
|
34
|
Yes
|
0
|
0
|
| |
Tyrphostin 47
|
2.4
|
No
|
No
|
85
|
No
|
0
|
0
|
| |
Tyrphostin 51
|
0.8
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
Tyrphostin AG1478
|
0.003
|
No
|
No
|
0
|
No
|
43
|
0
|
| |
Erbstatin (a)
|
0.77
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
Erlotinib
|
1
|
No
|
No
|
0
|
No
|
100
|
100
|
|
NGFRK
|
AG-879
|
10
|
No
|
No
|
100
|
No
|
22
|
0
|
|
EGFRK/CaMKII
|
Lavendustin C
|
2
|
No
|
No
|
0
|
No
|
0
|
0
|
|
CaMKII
|
KN-62
|
0.9
|
No
|
No
|
0
|
No
|
63
|
0
|
| |
KN-93
|
0.37
|
No
|
No
|
40
|
No
|
0
| |
|
MEK1/2
|
PD-98059
|
2
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
U-0126
|
0.072
|
No
|
No
|
0
|
No
|
0
|
0
|
|
p38MAPK
|
SB203580
|
0.07
|
No
|
No
|
0
|
No
|
0
|
0
|
|
PKA, PKG, MLCK, PKC
|
H-7
|
3.0
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
H-9
|
1.9
|
No
|
No
|
0
|
No
|
0
|
0
|
|
PKC
|
GF-109203X
|
0.02
|
Yes
|
No
|
100
|
No
|
100
|
0
|
| |
Hypericin
|
3.4
|
No
|
No
|
82
|
Yes
|
100
|
95
|
| |
Ro 31-8220
|
0.01
|
No
|
No
|
79
|
Yes
|
100
|
100
|
| |
Sphingosine
|
1-3
|
No
|
No
|
15*
|
No
|
0
|
0
|
| |
Palmitoyl-DL-
|
25
|
No
|
No
|
17*
|
No
|
0
|
0
|
| |
Carnitine-Cl
| | | | | | | |
|
PKCδ
|
Rottlerin
|
3-6
|
Yes
|
No
|
100
|
No
|
100
|
90
|
|
PKCα/γ
|
HBDDE
|
43
|
No
|
No
|
58
|
Yes
|
0
|
0
|
|
PKA
|
H-89
|
0.048
|
No
|
No
|
0
|
No
|
0
|
0
|
|
PKA/PKG
|
H-8
|
0.48
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
HA-1004
|
30
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
HA-1077
|
1.6
|
No
|
No
|
0
|
No
|
0
|
0
|
|
HER1-2
|
AG-825
|
0.35
|
No
|
No
|
43
|
Yes
|
0
|
0
|
|
Tyrosine
|
Tyrphostin AG1288
|
21
|
No
|
No
|
88
|
No
|
0
|
0
|
|
Kinases
|
Tyrphostin AG1295
|
25
|
No
|
No
|
0
|
No
|
0
|
0
|
| |
Genistein
|
0.002
|
No
|
No
|
0
|
No
|
0
|
0
|
|
IRK
|
HNMPA
|
10
|
No
|
No
|
0
|
No
|
0
|
0
|
|
JNK
|
SP 600125
|
0.04
|
No
|
No
|
0
|
No
|
0
|
0
|
|
p56 lck
|
Damnacanthal
|
0.017
|
No
|
No
|
0
|
No
|
47
|
0
|
|
Syk
|
Piceatannol
|
10
|
No
|
No
|
0
|
No
|
0
|
0
|
|
Src family
|
PP1
|
0.005
|
No
|
No
|
0
|
No
|
78
|
0
|
| |
PP2
|
0.004
|
No
|
No
|
0
|
No
|
100
|
45
|
|
JAK-2
|
AG-490
|
~5
|
No
|
No
|
0
|
No
|
0
|
0
|
|
ERK2, CK1, CK2
|
5-Iodotubercidin
|
0.4
|
No
|
No
|
0
|
No
|
100
|
100
|
|
cRAF
|
GW 5074
|
0.009
|
No
|
No
|
80
|
Yes
|
58
|
0
|
|
IKK pathway
|
BAY 11-7082
|
5
|
No
|
No
|
100
|
No
|
0
|
0
|
|
GSK-3β/CDK5
|
Indirubin-3'-monoxime
|
0.022
|
No
|
No
|
0
|
No
|
72
|
0
|
|
mTOR
|
Rapamycin
|
0.010
|
No
|
No
|
46
|
No
|
40
|
0
|
|
Neg. Cont. Tyr Kinase Inhibitor
|
Tyrphostin 1
|
NA
|
No
|
No
|
0
|
No
|
0
|
0
|
|
Neg. Cont. Genistein
|
Diadzein
|
NA
|
No
|
No
|
0
|
No
|
0
|
0
|
- The table summarizes data for the acidification assay using acridine orange (45 minute incubation) and the %-inhibition in the acid influx assay at 10 μM. It is stated whether the compounds quench the acridine orange signal. The %-inhibition in the bone resorption and AlamarBlue assay are also provided for each inhibitor tested. *Indicates auto fluorescence of the compound. Text in italics shows the compounds shown in the figures. # indicates lowest IC50 values obtained in relevant assays http://www.enzolifesciences.com. NA indicates not applicable (for negative controls).
