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. 2012 Sep 11;120(26):5103–5110. doi: 10.1182/blood-2012-07-444935

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.

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