5.30032

Nedd4/Rsp5 Signaling Inducer, NAB2

• 別名: Nedd4/Rsp5 Signaling Inducer, NAB2, N-(2-Chlorobenzyl)-1-(2,5-dimethylphenyl)-1H-benzo[d]imidazole-5-carboxamide
• 実験式（ヒル表記法）: C₂₃H₂₀ClN₃O
• CAS番号: 1504588-00-4
• 分子量: 389.88
• UNSPSCコード: 12352200
• PubChem Substance ID: 82017756
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C
• SMILES記法: CC1=CC(=C(C=C1)C)N2C=NC3=C2C=CC(=C3)C(=O)NCC4=CC=CC=C4Cl

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

注意

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.

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable