Rocaglamide

Synonyms: Roc-A

Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity.

Rocaglamide Chemical Structure

Rocaglamide Chemical Structure

CAS: 84573-16-0

Selleck's Rocaglamide has been cited by 2 publications

Purity & Quality Control

Batch: S742801 DMSO] 100 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.39%
99.39

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Biological Activity

Description Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity.
Targets
eIF4A [1] NF-κB [2] HSF1 [1]
(Cell-free assay)
50 nM
In vitro
In vitro

Rocaglamide A inhibits the heat shock reporter with IC50 of ~50 nM and inhibits the function of the translation initiation factor eIF4A, a DEAD box RNA helicase.[1] Rocaglamides are able to suppress the PMA-induced expression of NF-kappaB target genes and sensitize leukemic T cells to apoptosis induced by TNFalpha, cisplatin, and gamma-irradiation.[2]

Cell Research Cell lines MCF7 cells
Concentrations 200 nM
Incubation Time 6 hrs
Method

MCF7 cells are treated with 200 nM rocaglamide A for 6 hrs and RNA is then purified following extraction with TRIzol reagent. Gene expression analysis is performed using Affymetrix GeneChip HT Human Genome U133A 96-Array Plates.

In Vivo
In vivo

Rocaglamide induces apoptosis of tumor cells in SCID mice models. Rocaglamide has the potential to inhibit the growth of HCC cell-derived tumors in vivo.[3]

Animal Research Animal Models 6-week-old female SCID mice
Dosages 2.5 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 505.56 Formula

C29H31NO7

CAS No. 84573-16-0 SDF --
Smiles CN(C)C(=O)C1C(C2(C(C1O)(C3=C(O2)C=C(C=C3OC)OC)O)C4=CC=C(C=C4)OC)C5=CC=CC=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (197.8 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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