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蟛蜞菊内酯

选择性和不可逆的IκB激酶抑制剂
规格或纯度: ≥98%(HPLC)
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
W124219-1mg
1mg 现货 Stock Image
W124219-5mg
5mg 现货 Stock Image
W124219-25mg
25mg 现货 Stock Image
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CBR1 Inhibitor

基本描述

别名 7-甲氧基-5,11,12- 三羟基香豆素
英文别名 Wedelolactone|524-12-9|7-Methoxy-5,11,12-trihydroxycoumestan|7-Methoxy-5,11,12-trihydroxy-coumestan|IKK Inhibitor II|1,8,9-Trihydroxy-3-methoxycoumestan|CHEMBL97453|0K6L725GNS|CHEBI:10037|1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one|5,11,12
规格或纯度 ≥98%(HPLC)
英文名称 Wedelolactone
生化机理 Wedelolactone inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα. Irreversible inhibitor of IKKα and β kinase activity (IC50 < 10 μM). Wedelolactone has no effects on p38 MAP kinase or Akt.Selective and irreversible IκB kinase inhibitor. Inhibits osteoclastogenesis. Suppresses LPS-induced caspase 11 expression (IC 50 =35 µM). Shows hepatoprotective effects in vivo.
应用 Inhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis.
储存温度 2-8°C储存
运输条件 冰袋运输
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产品介绍

Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies sμggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies sμggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin, and galactosamine, and inhibit 5-lipoxygenase (5-LO)) activity in porcine leukocytes.Inhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis.

Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies suggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies suggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin, and galactosamine, and inhibit 5-lipoxygenase (5-LO)) activity in porcine leukocytes.
Inhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis.

名称和标识符

IUPAC Name 1,8,9-trihydroxy-3-methoxy-[1]benzofuro[3,2-c]chromen-6-one
INCHI InChI=1S/C16H10O7/c1-21-6-2-10(19)14-12(3-6)23-16(20)13-7-4-8(17)9(18)5-11(7)22-15(13)14/h2-5,17-19H,1H3
InChi Key XQDCKJKKMFWXGB-UHFFFAOYSA-N
Canonical SMILES COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O
Isomeric SMILES COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O
WGK Germany 3
PubChem CID 5281813
分子量 314.25

化学和物理性质

溶解性 Soluble in DMSO (25 mg/mL), and MeOH.
敏感性 对热敏感
熔点 315 °C

安全和危险性(GHS)

象形图
ghs07

Harmful

信号词 Warning
危险声明 H302: Harmful if swallowed
H317: May cause an allergic skin reaction
预防措施声明 P261,P280,P302+P352,P321,P501,P264,P270,P272,P333+P313,P362+P364,P330,P301+P317
WGK Germany 3
个人防护装备 dust mask type N95 (US), Eyeshields, Faceshields, Gloves

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