401480

IKK Inhibitor III, BMS-345541

IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM).

• 同義詞: IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
• 經驗公式（希爾表示法）: C₁₄H₁₇N₅ · 2C₂HF₃O₂
• CAS號碼: 445430-58-0
• 分子量：: 483.36
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥96% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated (hygroscopic); protect from light
• 顏色: off-white
• 溶解度: DMSO: 5 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• InChI: 1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18)
• InChI 密鑰: PSPFQEBFYXJZEV-UHFFFAOYSA-N

描述

一般說明

A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC₅₀ = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC₅₀ = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC₅₀ = 1-5 µM in THP-1 cells) and in vivo (IC₅₀ = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.

A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC₅₀ ~4.0 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC₅₀ = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC₅₀ = 1-5 µM in THP-1 cells) and in vivo (IC₅₀ = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.

生化／生理作用

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外觀

Supplied as bis-TFA salt.

其他說明

Townsend, R.M., et al. 2004. Transplantation77, 1090.
MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508.
McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652.
Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 1
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable