Rocaglamide Inhibitor

Name: Rocaglamide Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5764387
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5764387

Rocaglamide, isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-kappaB activation in T-cells. More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Rocaglamide, Inhibitor

Full Product Name

Rocaglamide

Product Synonym Names

Rocaglamide A

Form/Format

Solid. Powder

Preparation and Storage

Store at -20°C for 3 years.

Molecular Weight

505.56

Targets (IC50)

HSP,NF-κB,PERK

Solubility

DMSO: 10mg/mL (19.78mM)
Ethanol: 5mg/mL (9.89mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C29H31NO7

SMILES

CN(C)C([C@H]([C@H]([C@]1(c(cc2)ccc2OC)Oc2cc(OC)cc(OC)c2[C@]11O)c2ccccc2)[C@H]1O)=O

CAS Number

84573-16-0

Preparing Stock Solutions

1mM: 1.978mL (1mg); 9.890mL (5mg); 19.780mL (10mg)
5mM: 0.3956mL (1mL); 1.978mL (5mg); 3.956mL (10mg)
10mM: 0.1978mL (1mg); 0.989mL (5mg); 1.978mL (10mg)
50mM: 0.0396mL (1mg); 0.1978mL (5mg); 0.3956mL (10mg)
Please select the appropriate solvent to prepare the stock solution of the product in different solvents. Please use as soon as possible.

Cell Research

HepG2 and Huh-7 cells (1x10^4/well) are seeded in 96-well plates in complete culture medium and incubated for 24 hours. The cells are then exposed to 100nM Rocaglamide and/or 100ng/mL TRAIL for 24 hours. The control cells are treated with DMSO at a concentration equal to that used for the drug-treated cells. The complete culture medium is then removed and MTT (200 uL, 0.5mg/mL in 10% FBS-containing DMEM) is added to each well and the plate is incubated for 2 hours at 37 degree C in a humidified incubator. The solution is then removed from the wells and 200uL DMSO is added to each well prior to agitation. The absorbance at 570nM is read using a microplate reader (Bio-Tek ELx800). The value for the vehicle-treated cells is considered to indicate 100% viability. Furthermore, a crystal violet assay is carried out. Briefly, the cells (1x10^5/mL) are seeded in a 12 well plate for 12 h and treated with TRAIL (0-100ng/mL) and/or RocA(1-100nM) for 12 hours. The treated cells are washed with phosphate-buffered saline (PBS), fixed with 4% paraformaldehyde for 15 minutes, and stained using crystal violet for a further 30 min [2].

In Vitro

Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia [1,2,3]. treatment with Rocaglamide alone leads to apoptosis in 9% HepG2 and 11% Huh-7 cells and treatment with TRAIL induces apoptosis in 16% HepG2 and 17% Huh-7 cells. However, the combination of Rocaglamide and TRAIL induces apoptosis in 55% HepG2 and 57% Huh-7 cells, which is evidently more than an additive effect [2].

In vivo

Tumor volumes in the Rocaglamide-treated group are 45±12% compared with the control group. Rocaglamide significantly suppresses tumor growth compared with that in the control group. Treatment with Rocaglamide does not lead to any reduction in body weight and no apparent signs of toxicity are observed in the mice during the treatment [2].

Animal Research

The Huh-7 cells (3×10^6), suspended in 100 ?L mix (equal volumes of DMEM and Matrigel), are implanted subcutaneously into the right flank of 10 female SCID mice (6-week-old) and then randomly divided into two equal groups, one of which received an intraperitoneal injection of Rocaglamide (2.5 mg/kg in 80 ?L olive oil; n=5) and the other, used as a vehicle control, received olive oil alone (n=5). These treatments are performed once daily for 32 days and the tumor volumes and body weights of the animals are measured twice a week. The tumor volumes (mm3) are calculated using the following formula: Tumor volume=LS2/2, where L is the longest diameter and S is the shortest. At the end of the experiments, the mice are sacrificed and tumor samples are harvested, fixed in formalin and embedded in paraffin as tissue sections for immunohistochemical analysis [2].

Product Categories/Family for Rocaglamide, inhibitor

NF-kappab; NF-kappaB

Product References and Citations for Rocaglamide, inhibitor

Santagata S, et al. Tight coordination of protein translation and heat shock factor 1 activation supports the anabolic malignant state. Science. 2013 Jul 19; 341(6143): 1238303.
Santagata S, et al. Tight coordination of protein translation and heat shock factor 1 activation supports the anabolic malignant state. Science. 2013 Jul 19; 341(6143): 1238303.
Luan Z, et al. Rocaglamide overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells by attenuating the inhibition of caspase-8 through cellular FLICE-like-inhibitory protein downregulation. Mol Med Rep. 2015 Jan;11(1):203-11.
Luan Z, et al. Rocaglamide overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells by attenuating the inhibition of caspase-8 through cellular FLICE-like-inhibitory protein downregulation. Mol Med Rep. 2015 Jan;11(1):203-11.
Baumann B, et al. Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells. J Biol Chem. 2002 Nov 22;277(47):44791-800.
Baumann B, et al. Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells. J Biol Chem. 2002 Nov 22;277(47):44791-800.

Other Notes

Small volumes of Rocaglamide, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Rocaglamide purchase

MBS5764387 is an inhibitor targeting Rocaglamide.