Biochem/physiol Actions

Kd = 800 nM for calcineurin-NFAT

Reversible: no

Primary TargetCalcineurin-NFAT

Product does not compete with ATP.

Cell permeable: yes

General description

A cell-permeable, potent, and selective inhibitor of Calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling. Binds to calcineurin with high affinity (K_d = 800 nM), disrupts its interaction with NFAT, and completely blocks calcineurin-dependent NFAT dephosphorylation, nuclear import (~40 µM in C1.7W2 T cells), and induction of NFAT-targeted cytokine mRNAs. Unlike CsA (Cat. No. 239835) and FK506, INCA-6 does not affect calcineurin activity or its downstream signaling.

A cell-permeable quinone compound that acts as a potent and selective inhibitor of Calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling. Binds to calcineurin with high affinity (K_d = 800 nM), disrupts its interaction with NFAT and completely blocks its dephosphorylation, nuclear import of NFAT (~40 µM in C1.7W2 T cells), and induction of cytokine mRNAs. Unlike CsA (Cat. No. 239835) and FK506, INCA-6 does not affect calcineurin activity or its downstream signaling.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Roehrl, M.H.A., et al. 2004. Biochemistry43, 16067.Roehrl, M.H.A., et al. 2004. Proc. Natl. Acad. Sci. USA101, 7554.

Packaging

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)