Home ER stress & UPR HSP inhibitor - eIF inhibitor - NF-κB inhibitor Rocaglamide

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Rocaglamide HSP inhibitor

Cat.No.S7428

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. This compound inhibits the function of the translation initiation factor eIF4A. It also inhibits NF-κB activity. This chemical exhibits anti-tumor activity.
Rocaglamide HSP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 505.56

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 505.56 Formula

C29H31NO7

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 84573-16-0 -- Storage of Stock Solutions

Synonyms Roc-A 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
eIF4A [1]
NF-κB [2]
HSF1 [1]
(Cell-free assay)
50 nM
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] This compound is able to suppress the PMA-induced expression of NF-kappaB target genes and sensitize leukemic T cells to apoptosis induced by TNFalpha and gamma-irradiation.[2]
In vivo

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

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