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HERG-Lite® – Think Outside The Block
High Throughput, Non-Electrophysiological screening for hERG risk
Identify compounds that produce hERG risk by trafficking inihibition.
HERG-Lite is a chemiluminescent assay that monitors hERG expression at the cell surface. It identifies hERG trafficking inhibitors by exposing a wild-type (WT) hERG to drug overnight. HERG-Lite® identifies hERG channel blockers by measuring rescue of a trafficking-defective mutant hERG (SM) cell line.
Benefits:
- Only HERG-Lite detects compounds, such as anti-cancer drugs like arsenic trioxide and geldanamycin derivations that produce hERG risk indirectly by inhibiting trafficking
- HERG-Lite/TF assay detects trafficking inhibition and mature and immature hERG proteins
- Identifies compounds that block hERG directly and rescue the hERG SM cell line
- Results provided 48 hours after study completion
| Assay |
# TAs |
Protocol |
Concentrations |
Positive Control |
Negative Control |
| HERG-Lite® |
10 + |
3 conc. @ n=3, on SM & WT, plus pos. & neg. controls per group Turnaround time: 1 week |
1, 10 & 30 uM* @ n=3 per conc. *or your choice |
Astemizole* 1 conc. @ n=3 per group *or your choice |
DMSO 1 conc. @ n=6 per group |
| HERG-Lite®/TF |
5 + |
3 conc. @ n=3, on WT only Turnaround time: 1 week |
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| Drug |
Test Conc |
Relative Surface Expression |
hERG Risk |
| hERG SM |
hERG WT |
| Arsenic Trioxide |
1 |
1.04 |
0.86 |
Yes |
| 10 |
0.87 |
0.35 |
| Cisapride |
1 |
3.88 |
1.16 |
Yes |
| 10 |
5.05 |
1.19 |
| Quinidine |
1 |
1.22 |
0.97 |
Yes |
| 10 |
1.80 |
1.11 |
| Amiodarone |
1 |
1.51 |
0.99 |
Yes |
| 10 |
1.13 |
0.55 |
| Thioridazine |
1 |
0.98 |
0.92 |
Yes |
| 10 |
0.99 |
0.50 |
| Acetaminophen |
1 |
1.05 |
0.96 |
No |
| 10 |
1.06 |
0.96 |
| Aspirin |
1 |
0.97 |
0.98 |
No |
| 10 |
1.08 |
0.99 |
 SAB-HERG lite.pdf
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