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Description
Overview
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 NG-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.
Catalogue Number
538773
Brand Family
Calbiochem®
Synonyms
2-Amino-N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)acetamide Trifluoroacetate, NO Inhibitor, 8-Gly Carb
References
References
Grodzki, A.C., et al. 2015. J. Pharm. Exp. Ther.352, 438.
Grodzki, A.C., et al. 2015. J. Pharm. Exp. Ther.352, 438.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
28-July-2017 JSW
Synonyms
2-Amino-N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)acetamide Trifluoroacetate, NO Inhibitor, 8-Gly Carb
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 NG-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.
Form
Beige solid
Formulation
Supplied as a trifluoroacetate salt.
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₁₃H₁₁ClN₄O.CF₃CH₂O
Purity
≥98% by HPLC
Solubility
DMSO (25 mg/ml)
Storage
Protect from light
+2°C to +8°C
Hygroscopic
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Grodzki, A.C., et al. 2015. J. Pharm. Exp. Ther.352, 438.