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检测方案
≥98% (HPLC)
质量水平
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 50 mg/mL
储存温度
−20°C
SMILES字符串
CC1(C2=CCN3C(=O)N(C(=O)N3C2C4=C(O1)C=C(C=C4)O)C5=CC=CC=C5)C
一般描述
A cell-permeable, chromene-fused benzopyran-embedded tetracyclic compound that selectively and directly binds to the DNA binding domain box A of high mobility group box (HMGB) proteins and blocks their post-translational phosphorylation and acetylation. Diminishes the cytoplasmic accumulation of HMGB2 in microglial cells. Blocks lipopolysaccharide (LPS)-induced nitrite release in BV-2 microglial cells, RAW 264.7 macrophages, and mouse primary microglial cultures (~50 nM to 20 µM) without inducing any toxicity. However, it is shown to be less potent in primary astrocytes. Suppresses LPS-stimulated increase in the levels of IL-6, IL-1b, NOS2, and TNFα genes and inhibits the nuclear translocation of NF-κB. Also shown to reduce LPS-induced phosphorylation of ERK, JNK, and p38 MAP kinases in microglia. Reduces neuroinflammation, neurite damage, and spinal cord demyelination in a murine model of auto-immune encephalitis (~10 mg/kg).
A cell-permeable, chromene-fused benzopyran-embedded tetracyclic compound that selectively and directly binds to the DNA binding domain box A of high mobility group box (HMGB) proteins and blocks their post-translational phosphorylation and acetylation. Diminishes the cytoplasmic accumulation of HMGB2 in microglial cells. Blocks lipopolysaccharide (LPS)-induced nitrite release in BV-2 microglial cells, RAW 264.7 macrophages, and mouse primary microglial cultures (~50 nM to 20 µM) without inducing any toxicity. However, it is shown to be less potent in primary astrocytes. Suppresses LPS-stimulated increase in the levels of IL-6, IL-1b, NOS2, and TNFα genes and inhibits the nuclear translocation of NF-κB. Also shown to reduce LPS-induced phosphorylation of ERK, JNK, and p38 MAP kinases in microglia. Reduces neuroinflammation, neurite damage, and spinal cord demyelination in a murine model of auto-immune encephalitis (~10 mg/kg).
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
生化/生理作用
Cell permeable: yes
Primary Target
HMGB2
HMGB2
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Lee, S., et al. 2014. Nat. Chem. Biol.10, in press.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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