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Table 1 Summary of data for all inhibitors

From: Screening of protein kinase inhibitors identifies PKC inhibitors as inhibitors of osteoclastic acid secretion and bone resorption

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
  1. 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).