Table 1.
Coherence between sensor inducibility and cellular proliferation inhibition by the vitamin D3 analogues
| Vitamin D3 compound | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Calcitriol | Alfacalcidol | Atocalcitol | Calcipotriol | GS 1750 | GS 1590 | GS 1725 | KH 1230 | EB 1213 | |
| Relative IC50 -1 (1) | 1.0 | 1.1 | 1.6 | 2.9 | 2.9 | 32.3 | 35.7 | 76.9 | 250 |
| Relative potency (2) Clone #18 | 1.0 | 0.6 | 2.7 | 1.0 | 7.2 | 7.9 | 6.0 | 5.5 | 9.2 |
| Relative potency (2) Clone #7 | 1.0 | 3.3 | 4.2 | 3.3 | 9.1 | 13.5 | 12.7 | 8.9 | 13.2 |
(1) The half maximal inhibitory concentration (IC50) is a measure of the capability of the compounds to inhibit proliferation of HaCaT cells. For a direct comparison, the inverse value (IC50-1) is depicted here normalized to the response obtained during calcitriol exposure. IC50 values were measured for drug concentrations ranging from 10-11 to 10-7 M.
(2) The relative capacity of each compound to induce d2eGFP expression from the sensor is shown for each of the two clones #7 and #18 (data derived from figure 4). Induction of d2eGFP was measured at a drug concentration of 10-7 M.