Radicicol
(Synonyms: 根赤壳菌素; Monorden) 目录号 : GC11403An inhibitor of Hsp90
Sample solution is provided at 25 µL, 10mM.
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| Cell experiment [1]: | |
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Cell lines |
3T3-L1 preadipocytes |
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Preparation method |
The solubility of this compound in ethanol is 25 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
2.5, 5, and 10 μM |
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Applications |
In 3T3-L1 preadipocytes, radicicol dose-dependently reduced intracellular lipids, resulting in significantly lower lipid contents. Radicicol significantly decreased the protein expression of PPARγand C/EBPα protein, which then affected adipocyte differentiation. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6 mice |
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Dosage form |
60 mg/kg; diluted in vehicle (PBS) |
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Application |
In male C57BL/6 mice, radicicol (60 mg/kg) reduced cecal ligation and puncture (CLP)-induced leukocyte rolling by 15% and adhesion by 22%. In these septic mice, radicicol decreased CLP-induced MPO levels in the colon by 24%. Pretreatment with radicicol decreased CLP-evoked formation of MIP-2 and KC down to 68.4 ± 10.5 ng/g and 96.7 ± 15.2 ng/g, respectively, in the colon. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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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.
| Cas No. | 12772-57-5 | SDF | |
| 别名 | 根赤壳菌素; Monorden | ||
| 化学名 | (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 | ||
| Canonical SMILES | CC1CC2C(O2)C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1 | ||
| 分子式 | C18H17ClO6 | 分子量 | 364.78 |
| 溶解度 | 20mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。