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Radicicol

现货
Catalog No.
A4067
ATP酶/激酶抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 530.00
Ship with 10-15 days
5mg
¥ 2,450.00
Ship with 10-15 days

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Background

Radicicol is an inhibitor of the ATPase/kinase with IC50 values of <1μM, 100μM and 400μM, respectively for Hsp90, Topo VI and PDK3 [1].

Radicicol inhibits the activities of Hsp90, Topo VI and PDK3 by blocking ATP binding to them. Radicicol binds to the ATP-binding site in the C-terminal domain of PDK3 and competes with ATP. The inhibition does not cause the structure change of PDK3. Radicicol also shows a weak inhibition of PDK1 and PDK2 with IC50 value of 230mM and Ki value of 23μM, respectively [1].

As an inhibitor of Hsp90, radicicol is reported to downregulate the expression of PPARγ, C/EBPα , FAS and FABP4 results in the inhibition of lipid accumulation in 3T3-L1 adipocytes. Radicicol also has effects on cell cycle arrest and the PDK1/Akt pathway, thus causing the inhibition of the differentiation of 3T3-L1 preadipocytes. In addition, it is shown that radicicol increases the activation of the caspase-8- and Bid-dependent pathway and then enhances TRAIL-induced apoptosis in ovarian carcinoma cell lines [2, 3].

References:
[1] Kato M, Li J, Chuang JL, Chuang DT. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure. 2007 Aug;15(8):992-1004.
[2] He Y, Li Y, Zhang S, Perry B, Zhao T, Wang Y, Sun C. Radicicol, a heat shock protein 90 inhibitor, inhibits differentiation and adipogenesis in 3T3-L1 preadipocytes. Biochem Biophys Res Commun. 2013 Jun 28;436(2):169-74.
[3] Kim YJ, Lee SA, Myung SC, Kim W, Lee CS. Radicicol, an inhibitor of Hsp90, enhances TRAIL-induced apoptosis in human epithelial ovarian carcinoma cells by promoting activation of apoptosis-related proteins. Mol Cell Biochem. 2012 Jan;359(1-2):33-43.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt364.78
Cas No.12772-57-5
FormulaC18H17ClO6
SolubilitySoluble in ethanol
Chemical Name(2E,4E)-8-chloro-9,11-dihydroxy-14-methyl-15,15a-dihydro-1aH-benzo[c]oxireno[2,3-k][1]oxacyclotetradecine-6,12(7H,14H)-dione
SDFDownload SDF
Canonical SMILESCC1CC2C(O2)C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

3T3-L1前脂肪细胞

溶解方法

在乙醇中的溶解度为25mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

2.5, 5, and 10 μM

应用

在3T3-L1前脂肪细胞中,radicicol剂量依赖性地减少细胞内脂质,导致脂质含量显著降低。Radicicol显著降低PPARγ和C /EBPα蛋白的表达,从而影响脂肪细胞分化。

动物实验[2]:

动物模型

雄性C57BL / 6小鼠

剂量

60 mg/kg;在PBS中稀释

应用

在雄性C57BL / 6小鼠中,radicicol(60 mg/kg)将盲肠结扎穿刺(CLP)诱导的白细胞滚动减少15%,粘附减少22%。在这些脓毒症小鼠中,radicicol将结肠中CLP诱导的MPO水平降低了24%。Radicicol的预处理使结肠中CLP诱发的MIP-2和KC的形成分别降低至68.4±10.5ng / g和96.7±15.2ng / g。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] He Y, Li Y, Zhang S, Perry B, Zhao T, Wang Y, Sun C. Radicicol, a heat shock protein 90 inhibitor, inhibits differentiation and adipogenesis in 3T3-L1 preadipocytes. Biochem Biophys Res Commun. 2013 Jun 28;436(2):169-74.

[2]. Zhao Y, Huang ZJ, Rahman M, et al. Radicicol, an Hsp90 inhibitor, inhibits intestinal inflammation and leakage in abdominal sepsis. J Surg Res. 2013 Jun 15;182(2):312-8.

质量控制

质量控制和MSDS

批次:

化学结构

Radicicol