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 |
| 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).