Home>>Signaling Pathways>> Apoptosis>> Other Apoptosis>>Rottlerin
Rottlerin Catalog No.GC10820

PKC inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$72.00
In stock
50mg
$305.00
In stock

Customer Review

Based on customer reviews.

Tel: (626) 353-8530 Email: sales@glpbio.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:

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.

Chemical Properties

Cas No. 82-08-6 SDF
Synonyms N/A
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 100mM in DMSO Storage 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.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

Background

Rottlerin was originally identified as an inhibitor of PKCδ (IC50 = 3 μM), but can also inhibit CAM kinase III and a wide range of protein kinases, including PRAK and MAPKAP-K2 (IC50s = 1.9 and 5 μM, respectively).[1],[2] It can act as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1.[3] Rottlerin has also been shown to have neuroprotective effects in an MPTP animal model of Parkinson’s disease.[4]

Reference:

[1]. McGovern, S.L., and Shoichet, B.K. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).
[2]. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors Biochem. J. 351(1), 95-105 (2000).
[3]. Balgi, A.D., Fonseca, B.D., Donohue, E., et al. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling PLoS One 4(9), 1-15 (2009).
[4]. Zhang, D., Anantharam, V., Kanthasamy, A., et al. Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson’s disease Journal of Pharmacology and Experimental Therapeutics 322(3), 913-922 (2007).