General description
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 (Kd = 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.
A cell-permeable, potent, and selective inhibitor of Calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling. Binds to calcineurin with high affinity (Kd = 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.
Biochem/physiol Actions
Cell permeable: yes
Kd = 800 nM for calcineurin-NFAT
Primary Target
Calcineurin-NFAT
Product does not compete with ATP.
Reversible: no
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Roehrl, M.H.A., et al. 2004. Biochemistry43, 16067.
Roehrl, M.H.A., et al. 2004. Proc. Natl. Acad. Sci. USA101, 7554.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51283714
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 480403-5MG
