Rottlerin
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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1,2]: | |
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Cell lines |
Rat (C6) and two human gliomas (T98G and U138MG), glial cells, Rat lung microvascular endothelial cells, Rat primary pulmonary artery endothelial cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 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 |
24 h |
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Applications |
Rottlerin (24 h) decreased the growth of C6, T98G, and U138MG cells (IC50, 12 μM for C6 and >20 μM for T98G and Ui 38MG, respectively). Rottlerin (48 h) decreased the growth of C6, T98G, and Ui 38MG cells with the IC50 of 5, 7, and 9 μM, respectively. Rottlerin (5 μM) significantly reduced the number of S-phase cells in C6, T98G, and U138MG. In C6 cells, rottlerin treatment resulted in an accumulation of cytoplasmic vacuoles and packaging of cellular components within membranes. Rottlerin (5 μM) produced obvious DNA laddering in HL-60 human leukemia cells. Rottlerin dose-dependently increased basal endothelial monolayer permeability in rat LMVEC and PAEC. Rottlerin caused actomyosin filament and focal adhesion disruption. |
| Animal experiment [2]: | |
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Animal models |
Adult male Sprague-Dawley rats |
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Dosage form |
Intraperitoneal injection, 50 mg/kg |
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Application |
A dose response in EBD extravasation had been observed in animals treated with varying concentrations of Rottlerin. Rottlerin promoted rat lung edem. Rottlerin caused pulmonary edema in anesthesized rats via disruption of endothelial barrier function independent of hydrostatic changes. |
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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]. 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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