Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell-permeable carboline derived compound that acts as an inhibitor of both the constitutive (IC₅₀ = 7 µM) and the inducible (IC₅₀ = 7 µM and 20 µM for TNFalpha and LPS-induced) production of nitric oxide (⋅NO) in rat peritoneal macrophages in a manner independent of NF-κB activation. Only at higher concentrations (~ 100 µM), it inhibits NF-κB-mediated gene expression in differentiated THP1-XBlue cells. Shown to be about 40-fold more effective than N^G-nitro-L-arginine in inhibiting ⋅NO production and 15-fold more effective in blocking LPS-induced ⋅NO production. Does not affect LPS- or TNFalpha-mediated cytokine production in THP1-XBlue cells and has no effect on ERK1/2 and p38 phosphorylation in TNFalpha stimulated THP1-XBlue cells.

Legal Information

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

Other Notes

Grodzki, A.C., et al. 2015. J. Pharm. Exp. Ther.352, 438.

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

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

Warning

Toxicity: Standard Handling (A)