Rocaglamide, Inhibitor

Rocaglamide

Cat. Num. AAA5764387

• Purity: 98.00%
• Synonyms: Rocaglamide; Rocaglamide A; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• 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
• 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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Rocaglamide, inhibitor

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.

Product Categories/Family for Rocaglamide, inhibitor

NF-kappab; NF-kappaB

References

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.