5.30032

Nedd4/Rsp5 Signaling Inducer, NAB2

• Sinonimo/i: Nedd4/Rsp5 Signaling Inducer, NAB2, N-(2-Chlorobenzyl)-1-(2,5-dimethylphenyl)-1H-benzo[d]imidazole-5-carboxamide
• Formula empirica (notazione di Hill): C₂₃H₂₀ClN₃O
• Numero CAS: 1504588-00-4
• Peso molecolare: 389.88
• Codice UNSPSC: 12352200
• ID PubChem: 82017756
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: CC1=CC(=C(C=C1)C)N2C=NC3=C2C=CC(=C3)C(=O)NCC4=CC=CC=C4Cl

Descrizione

Descrizione generale

A cell-permeable N-aryl benzimidazole (NAB) compound that protects against α-synuclein (α-syn) toxicity in yeast (0.625 to 10 µM), wt human α-syn-expressing C. elegans dopaminergic (DA) neurons (10 µM), human A53T α-syn-expressing rat DA neurons (0.1 µM), as well as in human neurons differentiated from iPSCs derived from Parkinson′s disease (PD) patients carrying either AT53T α-syn or an α-syn triplication (5 to 40 µM) by restoring Nedd4 (mammalian)/Rsp5 (yeast) E3 ligase-dependent processes, including ER-to-Golgi, plasma membrane- and Golgi-to-vacuole/lysosome trafficking events, reducing α-syn-caused nitrosative and ER stress. NAB2 is also reported to inhibit the growth, but not viability, of non-α-syn-expressing yeast via the same mechanism of action (MOA) albeit at a lower potency (GI₄₀ = 20.5 µM vs. EC₄₀ = 4.5 µM against α-syn toxicity). Although the exact molecular mechanism is yet unknown, NAB2 does not affect cellular α-syn level or Nedd4/Rsp5 ligase activity.

A cell-permeable N-aryl benzimidazole (NAB) compound that protects against α-synuclein (α-syn) toxicity in yeast (0.625 to 10 µM), wt human α-syn-expressing C. elegans dopaminergic neurons (10 µM), human A53T α-syn-expressing rat DA neurons (0.1 µM), as well as in Parkinson′s disease patients-derived neurons carrying AT53T α-syn or an α-syn triplication (5 to 40 µM) by restoring Nedd4 (mammalian)/Rsp5 (yeast) E3 ligase-dependent trafficking events, reducing α-syn-caused nitrosative and ER stress without affecting cellular α-syn level or Nedd4/Rsp5 ligase activity.

A cell-permeable compound that protects against alpha-synuclein toxicity.

Azioni biochim/fisiol

Cell permeable: yes

Avvertenza

NAB2 is moderately hydrophobic (clogP ~5.2)and can precipitate out of solution if added directly to cell culture or yeast media. Care should therefore be taken to optimize solubility and guard against false negative results caused by irrecoverable precipitation of the compound. Please refer to the Recommended Reaction Conditions above for details.

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

Tardiff, D.F., et al. 2013. Science342, 979.
Chung, C.Y., et al. 2013. Science342, 983.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable