c-Rel Inhibitor, IT-603-Calbiochem

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一般描述

A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC₅₀= 3 ?M in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC₅₀= 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).
A cell-permeable benzylidene-thioxo-imidazolidinone compund that directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity (IC₅₀= 3 ?M in EMSA). Shows good selectivity over Oct1 and AP1. Reduces IL-2 expression in activated T cells without affecting their viability. Induces growth arrest in diffuse large B-cell lymphoma (DLBCL) cell line Ly3 (IC₅₀= 18 uM). Shown to reduce alloactivation in T cells and diminish graft-versus-host disease (GVHD), but does not impair TCR-mediated killing. Improves the survival rate of lethally irradiated BABL/c mice transplanted with T cell depleted bone marrow cells from C57BL/6 mice (~24 mg/kg, i.p, daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Primary Target
c-Rel
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Use only fresh DMSO for reconstitution.
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Shono, Y., et al. 2014.Cancer Discovery4,578.

法律信息

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

基本信息

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安全信息