Rottlerin
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.
Rottlerin is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM[1].
Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner and exhibits cell proliferation in HMVEC[2].
In Balb C nude mice, rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth with no toxicity. Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].
References:
[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun, 1994, 199(1): 93-8.
[2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des, 2011, 77(6): 460-70.
[3]. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters, 2014, 353(1): 32-40.
- 1. Dong Y, Gao J, et al. "Antigen-Conjugated Silica Solid Sphere as Nanovaccine for Cancer Immunotherapy." Int J Nanomedicine. 2020;15:2685-2697. PMID:32368049
- 2. Wei P, Ning M, et al. "Spiroplasma eriocheiris entered Drosophila Schneider 2 cells and relied on clathrin-mediated endocytosis and macropinocytosis." Infect Immun. 2019 Aug 26. pii: IAI.00233-19. PMID:31451616
- 3. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
| Physical Appearance | A yellow to orange solid |
| Storage | Store at -20°C |
| M.Wt | 516.55 |
| Cas No. | 82-08-6 |
| Formula | C30H28O8 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥23.6 mg/mL in DMSO |
| Chemical Name | (Z)-1-(6-(3-acetyl-2,4,6-trihydroxy-5-methylbenzyl)-5,7-dihydroxy-2,2-dimethyl-2H-chromen-8-yl)-3-phenylprop-2-en-1-one |
| SDF | Download SDF |
| Canonical SMILES | OC1=C2C(OC(C)(C)C=C2)=C(C(/C=C\C3=CC=CC=C3)=O)C(O)=C1CC(C(O)=C(C)C(O)=C4C(C)=O)=C4O |
| 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[1,2]: | |
|
细胞系 |
大鼠（C6）和两种人神经胶质瘤（T98G和U138MG）细胞，神经胶质细胞，大鼠肺微血管内皮细胞，大鼠原发性肺动脉内皮细胞 |
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溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
|
反应条件 |
24 h |
|
应用 |
Rottlerin（24小时）降低了C6、T98G和U138MG细胞的生长，C6的IC50为12 μM，T98G和Ui 38MG的IC50为大于20 μM，Rottlerin（48h）降低了C6、T98G和Ui38MG细胞的生长，IC50分别为5、7和9 μM，Rottlerin（5 μM）显著降低C6、T98G和U138MG中S期细胞的数量。在C6细胞中，Rottlerin导致细胞质空泡的积累和细胞组分在膜内的包装。在HL-60人白血病细胞中，Rottlerin（5 μM）产生明显的DNA梯度，Rottlerin以剂量依赖的方式显著增加大鼠LMVEC和PAEC中的基底内皮单层通透性，Rottlerin引起肌动球蛋白丝和局灶粘连中断。 |
| 动物实验[2]: | |
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动物模型 |
成年雄性Sprague-Dawley大鼠 |
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给药剂量 |
腹腔注射，50 mg/kg |
|
应用 |
在用不同浓度的Rottlerin处理的动物中，观察到EBD外渗的剂量反应。Rottlerin促进大鼠肺水肿。在麻醉大鼠中，Rottlerin通过独立于静水压变化破坏内皮屏障功能引起肺水肿。 |
|
注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
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References: [1]. Parmer T G, Ward M D, Hait W N. Effects of rottlerin, an inhibitor of calmodulin-dependent protein kinase III, on cellular proliferation, viability, and cell cycle distribution in malignant glioma cells[J]. Cell growth & differentiation: the molecular biology journal of the American Association for Cancer Research, 1997, 8(3): 327-334. [2]. Klinger J R, Murray J D, Casserly B, et al. Rottlerin causes pulmonary edema in vivo: a possible role for PKCδ[J]. Journal of applied physiology, 2007, 103(6): 2084-2094. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
