Table 1.
Panel of cationic compounds, polymers, and proteins
Compound | No.* | IC50 (or % inhibition)* |
---|---|---|
Low MW polyethyleneimine | 1 | 10 ng/mL |
Polybrene | 2 | 19 ng/mL |
High MW polyethyleneimine | 3 | 35 ng/mL |
Generation 3.0 dendrimer | 40 ng/mL | |
Generation 2.0 dendrimer | 47 ng/mL | |
Norspermine | 52 ng/mL | |
Spermine | 4 | 57 ng/mL |
Generation 1.0 dendrimer | 5 | 58 ng/mL |
Histone H1 | 6 | 59 ng/mL |
Poly-D-lysine | 79 ng/mL | |
Poly-L-arginine | 81 ng/mL | |
Protamine sulfate | 8 | 0.11 μg/mL |
Poly-L-lysine | 0.14 μg/mL | |
Generation 0.0 dendrimer | 0.14 μg/mL | |
Heparin | 0.27 μg/mL | |
Polymyxin B | 9 | 0.38 μg/mL |
Histone H2A/H2B dimer | 0.38 μg/mL | |
Histone H2B | 0.46 μg/mL | |
Histone H3.1/H4 tetramer | 0.53 μg/mL | |
Histone H4 | 0.84 μg/mL | |
Colistin | 0.91 μg/mL | |
Histones (mixed) | 0.93 μg/mL | |
Histone H2A | 1.3 μg/mL | |
Spermidine | 1.7 μg/mL | |
Histone H3.1 | 2.5 μg/mL | |
Human platelet factor 4 | 10 | 3.8 μg/mL |
PPXbd | 11 | 8.5 μg/mL |
Lon protease polyP-binding domain | 72 μg/mL | |
1,3-diaminopropane | 0.47 mg/mL | |
Ethylenediamine | 0.89 mg/mL | |
Norspermidine | (62% inhibition at 200 μg/mL) | |
1,2-bis(3-aminopropylamino)ethane | (53% inhibition at 200 μg/mL) | |
Kanamycin | (48% inhibition at 200 μg/mL) | |
DNase I | (36% inhibition at 200 μg/mL) | |
RNase A | (23% inhibition at 100 μg/mL) | |
Bacitracin | (12% inhibition at 200 μg/mL) | |
Methylenediamine | (73% inhibition at 6 mg/mL) | |
Ammonium chloride | (44% inhibition at 2.7 mg/mL) | |
Melamine | (0% inhibition at 200 μg/mL) | |
Cystamine | (0% inhibition at 200 μg/mL) | |
Histamine | (0% inhibition at 200 μg/mL) | |
Histidine | (0% inhibition at 200 μg/mL) |
Each substance was tested at 200 μg/mL (or indicated concentrations) for inhibition of thrombin binding to immobilized biotin-polyP. Those exhibiting > 70% inhibition were retested at various inhibitor concentrations, from which IC50 values were derived (listed here in order of decreasing potency).
Numbers are the compound numbers used in Figure 2.