506282

Cl-amidine

>95% (HPLC), solid, PAD inhibitor, Calbiochem^®

• 別名: PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
• 実験式（ヒル表記法）: C₁₆H₂₀ClF₃N₄O₄
• 分子量: 424.80
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• product name: PAD Inhibitor, Cl-amidine, Cl-amidine is a cell-permeable pan PAD inhibitor (IC₅₀ = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively). Inactivates the calcium bound form of PAD4 in an irreversible manner.
• 品質水準: 200
• アッセイ: >95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

A cell-permeable compound that acts as a pan PAD inhibitor (IC₅₀ = 0.8 µM, 6.2 µM and 5.9 µM for PAD1, PAD3, and PAD4, respectively) in enzymatic assays. It preferentially inactivates the calcium bound form of PAD4 in an irreversible manner, and is shown to complete with BAEE for the active site residue of this enzyme. A small but significant reduction in the efficiency of p300GDB-GRIP1 interaction is observed in transiently transfected CV-1 cells treated with Cl-amidine at concentrations between 25 µM and 200 µM, in vivo. Furthermore, this compound (200 µM) together with HDAC inhibitor SAHA (0.4 µM) has shown additive effects in inducing p21, GADD45, and PUMA expression and inhibiting cancer cell growth in a p53-dependent manner in U2OS cells.

警告

Toxicity: Regulatory Review (Z)

再構成

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

その他情報

Knuckley, B., et al. 2010. Biochemistry23, 4852.
Li, P., et al. 2010. Oncogene21, 3153.
Luo, Y., et al. 2006. Biochemistry39, 11727.

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