Drug intelligence / Profile preview

calyculin a

Development stage
Discontinued
Modality
Small Molecules
Administration
Laboratory Use Only (not Administered Clinically)
01

Overview

Calyculin A is a highly potent and cell-permeable inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A), isolated from the marine sponge Discodermia calyx. It acts at nanomolar concentrations (IC50 for PP1 ≈ 2 nM; IC50 for PP2A ≈ 0.5–1 nM) and is widely used in biological research to study phosphorylation-dependent signaling pathways[2][3][5]. Mechanistically, it binds to the catalytic subunits of serine/threonine protein phosphatases PP1 and PP2A, inhibiting their activity and thereby increasing cellular phosphorylation levels[3][10]. Calyculin A is also recognized as a potent tumor promoter in experimental models due to its ability to induce hyperphosphorylation of proteins involved in cell growth regulation[10]. It is not approved for clinical use or marketed as a pharmaceutical drug; its applications are strictly limited to laboratory research.

Other names
Calyculin A(-)-Calyculin Acalyculin a from discodermia calyxC05370C-05370C 05370
02

Targets

PP1 (Protein phosphatase 1)PP2A (Protein phosphatase 2A)

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