5.33162

RAN Translation Inhibitor, NSC311153

• Synonym(s): RAN Translation Inhibitor, NSC311153, 9-Hydroxy-5,11-dimethyl-2-(2-(piperidin-1-yl)ethyl)-6H-pyrido[4,3-b]carbazol-2-ium Bromide, HBr, 9-Hydroxy-5,11-dimethyl-2-(2-(piperidyl)ethyl)-6H-pyrido(4,3-b)carbazolium Bromide, HBr, (GGGGCC)exp RNA Inhibitor, NSC-311153, NSC 311153
• Empirical Formula (Hill Notation): C₂₄H₂₈BrN₃O · xHBr
• Molecular Weight: 454.40 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥96% (HPLC)
• Quality Level: 100
• form: solid
• potency: 9.7 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: orange
• solubility: water: 5 mg/mL; DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell permeable indole fused isoquinolinium salt that binds to the expanded repeat (r(GGGGCC)exp (K_d = 9.7 µM) with modest selectivity. This binding is dependent upon the ionic strength and appears to be significantly weaker in the presence of Na+ and K+. Inhibits repeat-associated non-ATG (RAN) translation and foci Formation in r(GGGGCC)66-expressing HEK293 cells and reduces the levels of poly(GP) and poly(GA) proteins (10% at 25 µM; 47% at to 100 µM). Also shown to inhibit RAN translation and foci formation in (GGGGCC)exp-expressing C9ORF72+ iNeurons (~ 2 µM).

A cell permeable indole fused isoquinolinium salt that binds to the expanded repeat (r(GGGGCC)exp (K_d = 9.7 µM) with modest selectivity. This binding is dependent upon the ionic strength and appears to be significantly weaker in the presence of Na+ and K+. Inhibits repeat-associated non-ATG (RAN) translation and foci Formation in r(GGGGCC)66-expressing HEK293 cells and reduces the levels of poly(GP) and poly(GA) proteins (10% at 25 µM; 47% at to 100 µM). Also shown to inhibit RAN translation and foci formation in (GGGGCC)exp-expressing C9ORF72+ iNeurons (~ 2 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
(r(GGGGCC)exp

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as HBr salt.

Reconstitution

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

Other Notes

Su, Z., et al. 2014. Neuron.83, 1043.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable