In vitro inhibition of polyP activity by selected UHRA compounds
| Compound . | Size (kDa) . | No. of R groups . | Thrombin binding . | Plasma clotting assay . | ||||
|---|---|---|---|---|---|---|---|---|
| IC50 . | ECdouble polyP . | ECdouble RNA . | ||||||
| nM . | ng/mL . | nM . | µg/mL . | µM . | µg/mL . | |||
| UHRA-8 | 23 | 24 | 5.4 ± 1.8 | 124 ± 41 | 52 ± 15 | 1.20 ± 0.34 | 0.62 ± 0.21 | 14 ± 4.8 |
| UHRA-9 | 16 | 16 | 7.6 ± 2.0 | 122 ± 32 | 80 ± 16 | 1.28 ± 0.26 | 1.9 ± 0.59 | 30 ± 9.4 |
| UHRA-10 | 10 | 11 | 7.3 ± 3.7 | 73 ± 37 | 132 ± 38 | 1.32 ± 0.38 | 2.0 ± 0.58 | 20 ± 5.8 |
| UHRA-14 | 10 | 7 | 6.6 ± 2.4 | 66 ± 24 | 92 ± 13 | 0.92 ± 0.13 | 2.2 ± 0.65 | 22 ± 6.5 |
| Compound . | Size (kDa) . | No. of R groups . | Thrombin binding . | Plasma clotting assay . | ||||
|---|---|---|---|---|---|---|---|---|
| IC50 . | ECdouble polyP . | ECdouble RNA . | ||||||
| nM . | ng/mL . | nM . | µg/mL . | µM . | µg/mL . | |||
| UHRA-8 | 23 | 24 | 5.4 ± 1.8 | 124 ± 41 | 52 ± 15 | 1.20 ± 0.34 | 0.62 ± 0.21 | 14 ± 4.8 |
| UHRA-9 | 16 | 16 | 7.6 ± 2.0 | 122 ± 32 | 80 ± 16 | 1.28 ± 0.26 | 1.9 ± 0.59 | 30 ± 9.4 |
| UHRA-10 | 10 | 11 | 7.3 ± 3.7 | 73 ± 37 | 132 ± 38 | 1.32 ± 0.38 | 2.0 ± 0.58 | 20 ± 5.8 |
| UHRA-14 | 10 | 7 | 6.6 ± 2.4 | 66 ± 24 | 92 ± 13 | 0.92 ± 0.13 | 2.2 ± 0.65 | 22 ± 6.5 |
Results are 50% inhibitory concentration (IC50) for inhibiting thrombin binding to immobilized polyP (n = 5); and ECdouble (concentration needed to double the clotting time) in plasma clotting assays initiated with either 10 μM long-chain polyP (ECdouble polyP, n = 3) or 25 µg/mL polyguanylic acid (ECdouble RNA, n = 3). Data are reported in terms of both molarity and mass/volume ± standard error of the mean.