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

9,10-DIHYDRO-9,10[1',2']-BENZENOANTHRACENE-1,4-DIONE 화학적 특성, 용도, 생산

• 개요

  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.

• 용도

  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.

• 일반 설명

  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.

• 생물학적 활성

  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.

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