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Table 1 Sigma-2 binding affinity and pancreatic cancer cell line viability, following sigma-2 receptor ligand treatment (24 h)

From: Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer

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

  1. 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