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RottlerinPKC inhibitor

Rottlerin

Catalog No. B6803
Size Price Stock Qty
10mM (in 1mL DMSO) $80.00 In stock
10mg $98.00 In stock
50mg $424.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Rottlerin

Protocol

Cell experiment [1,2]:

Cell lines

Rat (C6) and two human gliomas (T98G and U138MG), glial cells, Rat lung microvascular endothelial cells, Rat primary pulmonary artery endothelial cells

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.

Reacting condition

24 h

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]:

Animal models

Adult male Sprague-Dawley rats

Dosage form

Intraperitoneal injection, 50 mg/kg

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.

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.

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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Chemical Properties

Cas No. 82-08-6 SDF Download SDF
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
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
Formula C30H28O8 M.Wt 516.55
Solubility Soluble in DMSO > 10 mM Storage Store at +4°C
General tips N/A
Shipping Condition N/A