Psora 4

Biological Activity

Psora 4 is a potent K_V1.3 channel blocker (EC₅₀ = 3 nM). Preferentially binds the C-type inactivated state of the channel, similar to the activity of CP 339818 (Cat. No. 1399). Displays 17- to 70-fold selectivity over closely-related K_V1 channels (K_V1, K_V2, K_V4 and K_V7); exhibits activity at K_V1.5 (IC₅₀ = 7.7 nM). Suppresses proliferation of human and rat myelin-specific effector memory T cells (EC₅₀ values are 25 and 60 nM respectively).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Voltage-gated potassium channel Kv1.3 regulates GLUT4 trafficking to the plasma membrane via a Ca²⁺-dependent mechanism.
   Li et al.
   Am.J.Physiol.Cell Physiol., 2006;290:C345
2. Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators.
   Vennekamp et al.
   Mol.Pharmacol., 2004;65:1364
3. Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases.
   Schmitz et al.
   Mol.Pharmacol., 2005;68:1254

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