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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)

CAS编号: 524-12-9
分子式: C₁₆H₁₀O₇
分子量: 314.25
MDL号: MFCD07778564
PubChem编号: 5281813

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货号 (SKU)	包装规格	是否现货
W124219-1mg	1mg	现货
W124219-5mg	5mg	现货
W124219-25mg	25mg	现货

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CBR1 Inhibitor

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基本描述

规格或纯度	≥98%(HPLC)
英文名称	Wedelolactone
别名	7-甲氧基-5,11,12- 三羟基香豆素
英文别名	1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c][1]benzopyran-6-one; 7-Methoxy-5,11,12-trihydroxycoumestan;IKK Inhibitor II; Eclipta alba
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
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
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
分子式	C₁₆H₁₀O₇
PubChem CID	5281813
分子量	314.25

数据库链接

Wikipedia	Wedelolactone
CAS Registry No.	524-12-9
PubChem CID	5281813
ChEMBL Ligand	CHEMBL97453
ChEBI	CHEBI:10037

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

安全信息

象形图	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

靶标

Target ID

1383

名称

CBR1

缩写名

SHP2

家族

Prostaglandin synthases

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	277	21q22.12	CBR1	carbonyl reductase 1
Mouse	2	277	16 54.53 cM	Cbr1	carbonyl reductase 1
Rat	2	277	11q11	Cbr1	carbonyl reductase 1

Ensembl Gene

ENSG00000159228 (Hs) , ENSMUSG00000051483 (Mm) , ENSRNOG00000047848 (Rn) , ENSRNOG00000049693 (Rn) , ENSRNOG00000049911 (Rn)

Entrez Gene

12408 (Mm) , 29224 (Rn) , 873 (Hs)

OMIM

114830 (Hs)

Protein GI

4502599 (Hs) , 113680352 (Mm) , 9506467 (Rn)

UniProtKB

P16152 (Hs) , P48758 (Mm) , P47727 (Rn)

ChEMBL Target

CHEMBL5586 (Hs)

关联配体

Ligand ID	5551
名称	wedelolactone
类别	Natural product
学名	1,8,9-trihydroxy-3-methoxy-[1]benzoxolo[3,2-c]chromen-6-one
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	Found in Eclipta alba (false daisy) and in Wedelia calendulacea.