Radicicol
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Radicicol是一种ATP酶/激酶抑制剂，对Hsp90、Topo VI和PDK3的IC50值分别为小于1 μM、100 μM和400 μM[1]。
Radicicol可通过阻断ATP结合，抑制Hsp90、Topo VI和PDK3的活性。Radicicol可与PDK3的C端结构域的ATP结合位点结合，与ATP竞争。此种抑制不会导致PDK3结构变化。Radicicol对PDK1和PDK2也具有较弱的抑制能力，对应的IC50值和Ki值分别为230 mM和23 μM[1]。
作为Hsp90的抑制剂，radicicol可下调PPARγ、C/EBPα、FAS和FABP4的表达，导致3T3-L1脂肪细胞中脂肪积累的抑制。Radicicol对细胞周期停滞和PDK1/Akt途径也有效果，进而引起3T3-L1前脂肪细胞的分化抑制。此外，radicicol可在卵巢癌细胞系中增加caspase-8和Bid依赖途径的激活，提高TRAIL诱发的细胞凋亡[2,3]。
参考文献：
[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.
- 1. Yu Zheng, Yingying Tao, et al. "Nuclear receptor 4A1 (NR4A1) silencing protects hepatocyte against hypoxia-reperfusion injury in vitro by activating liver kinase B1 (LKB1)/AMP-activated protein kinase (AMPK) signaling." Bioengineered. 2022 Apr;13(4):8349-8359. PMID: 35311465
- 2. Xu J, Shi Q, et al. "Metabolic enzyme PDK3 forms a positive feedback loop with transcription factor HSF1 to drive chemoresistance." Theranostics. 2019 May 9;9(10):2999-3013. PMID: 31244938
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 364.78 |
| Cas No. | 12772-57-5 |
| Formula | C18H17ClO6 |
| Solubility | Soluble 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1CC2C(O2)C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
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细胞系 |
3T3-L1前脂肪细胞 |
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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。 |
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反应条件 |
2.5, 5, and 10 μM |
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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]: | |
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动物模型 |
雄性C57BL / 6小鼠 |
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剂量 |
60 mg/kg;在PBS中稀释 |
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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。 |
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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。 |
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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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化学结构
相关生物数据
相关生物数据
