Table 2.
Results of the chaperone assay for amodiaquine, chrysin, and lead compounds from study by Heinrich et al.14 in comparison to the control BVDU.
| Compound | Dosage | Rel. CS Precip. | Rel. Inhib. | |
|---|---|---|---|---|
| PLIP Screening | Chrysin | 10 μM | 0.92 | 69x |
| Amodiaquine | 10 μM | 0.57 | 43x | |
| Heinrich et al. | CAS 50-53-3 | 10 μM | 1.06 | 80x |
| CAS 61-00-7 | 10 μM | 0.99 | 74x | |
| CAS 104715-80-2 | 10 μM | 0.92 | 69x | |
| CAS 1222781-87-4 | 10 μM | 0.81 | 61x | |
| CAS 161363-17-3 | 10 μM | 0.71 | 53x | |
| CAS 1222812-38-5 | 10 μM | 0.65 | 49x | |
| CAS 53-86-1 | — | — | — | |
| Control | BVDU | 750 μM | 1 | 1x |
Listed are the dosage used in the experiment, the relative precipication of the client protein citrate synthase, and the relative inhibition after correcting for the dosage. Amodiaquine is substantially better than BVDU in inhibition of Hsp27 chaperone activity and within the activity range of compounds identified by Heinrich et al.14. The same is true for chrysin.