Cmpd | Affinity (K
i, nM) | Activity (EC50, μM) |
---|
 | σ2
| Panc02 | KP02 | KCKO | MIAPaCa-2 | BxPC3 | AsPC-1 | Panc-1 |
---|
PB28a
| 0.68 | 43 | >100 | 87 | 51 | >100 | >100 | >100 |
PB221a
| 18.8 | 37 | >100 | 19 | 50 | 100 | >100 | >100 |
PB183b
| 9.24 | 83 | 97 | 51 | 49 | 100 | >100 | >100 |
F281c
| 12.6 | 37 | 49 | 62 | 29 | 42 | 98 | >100 |
PB282d
| 14.1 | >100 | >100 | 90 | 51 | >100 | >100 | >100 |
-
aSigma-2 binding data are from Berardi, et al. 2009 [26]; bSigma-2 binding data are from Berardi, et al. 2004 [25]; cSigma-2 binding data are from Ferorelli et al., 2007 [27]; dSigma-2 binding data are from Abate, et al., 2011 [28]. Pancreas cancer cell lines were treated with escalating doses of the sigma-2 ligands PB28, PB221, PB183, F281, PB282 or DMSO vehicle for 24 h and viability relative to vehicle determined by MTT Assay