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).
别名:
IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
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About This Item
推荐产品
品質等級
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
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.
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
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
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