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) |
| 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.