Table 1 Summary of data for all inhibitors
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 |
| Â | AG-1296 | 1 | No | No | 15 | Yes | 0 | 0 |
EGFRK/PDGFRK | AG-494 | 1.2 | No | No | 55 | No | 0 | 0 |
| Â | Tyrphostin 46 | 9.2 | No | No | 0 | No | 0 | 0 |
EGFRK | Lavendustin A | 0.011 | No | No | 0 | No | 0 | 0 |
| Â | RG-14620 | 3 | No | No | 0 | No | 0 | 0 |
| Â | Tyrphostin 23 | 35 | No | No | 45 | Yes | 0 | 0 |
| Â | Tyrphostin 25 | 3 | No | No | 34 | Yes | 0 | 0 |
| Â | Tyrphostin 47 | 2.4 | No | No | 85 | No | 0 | 0 |
| Â | Tyrphostin 51 | 0.8 | No | No | 0 | No | 0 | 0 |
| Â | Tyrphostin AG1478 | 0.003 | No | No | 0 | No | 43 | 0 |
| Â | Erbstatin (a) | 0.77 | No | No | 0 | No | 0 | 0 |
| Â | 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 |
| Â | KN-93 | 0.37 | No | No | 40 | No | 0 | Â |
MEK1/2 | PD-98059 | 2 | No | No | 0 | No | 0 | 0 |
| Â | 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 |
| Â | H-9 | 1.9 | No | No | 0 | No | 0 | 0 |
PKC | GF-109203X | 0.02 | Yes | No | 100 | No | 100 | 0 |
| Â | Hypericin | 3.4 | No | No | 82 | Yes | 100 | 95 |
| Â | Ro 31-8220 | 0.01 | No | No | 79 | Yes | 100 | 100 |
| Â | Sphingosine | 1-3 | No | No | 15* | No | 0 | 0 |
| Â | Palmitoyl-DL- | 25 | No | No | 17* | No | 0 | 0 |
| Â | Carnitine-Cl | Â | Â | Â | Â | Â | Â | Â |
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 |
| Â | HA-1004 | 30 | No | No | 0 | No | 0 | 0 |
| Â | 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 |
| Â | 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 |
| Â | 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 |