9,10-DIHYDRO-9,10[1',2']-BENZENOANTHRACENE-1,4-DIONE

Description

NFAT activation inhibitor III is a cell-permeant inhibitor of signaling through nuclear factor of activated T cells (NFAT). It binds the substrate recognition site of the phosphatase calcineurin (K_d = 0.8 μM), preventing it from binding and dephosphorylating NFAT. NFAT activation inhibitor III blocks the nuclear import of NFAT in T cells stimulated with ionomycin . It prevents the induced expression of cytokine mRNAs in T cells stimulated with phorbol ester and ionomycin.

The Uses of 9,10-DIHYDRO-9,10[1',2']-BENZENOANTHRACENE-1,4-DIONE

INCA 6 inhibits nuclear factor of activated T cells (NFAT) dephosphorylation and nuclear import, which in turn, interferes with downstream targets of NFAT including induction of cytokine mRNAs.

What are the applications of Application

NFAT Activation Inhibitor III is a potent and selective calcineurin-NFAT signaling inhibitor

Definition

ChEBI: LSM-2729 is an anthraquinone.

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.

Biological Activity

Inhibitor of interaction between calcineurin and its substrate nuclear factor of activated T cells (NFAT); blocks at the substrate recognition site but not at the catalytic site (K d = 0.8 mM). Inhibits NFAT dephosphorylation and nuclear import. Also prevents induction of cytokine mRNAs that are downstream targets of NFAT.

Biochem/physiol Actions

Cell permeable: yes

storage

Store at -20°C