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Rocaglamide HSP inhibitor

Name: Rocaglamide
Brand: Selleck Chemicals
SKU: S7428
Rating: 5 (3 reviews)

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.

Chemical Structure

Molecular Weight: 505.56

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.39

Related Targets	JNK Antioxidant ROS eIF PERK IRE1 PKR ASK PDI ATF-6
Other HSP Inhibitors	Tanespimycin (17-AAG) Elesclomol (STA-4783) Luminespib (NVP-AUY922) Ganetespib (STA-9090) Alvespimycin (17-DMAG) Hydrochloride VER-155008 Onalespib (AT13387) BIIB021 Zelavespib (PU-H71) HSP990 (NVP-HSP990)

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	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	eIF4A NF-κB HSF1 (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. This compound is able to suppress the PMA-induced expression of NF-kappaB target genes and sensitise leukemic T cells to apoptosis induced by TNFalpha and gamma-irradiation.
In vivo	Rocaglamide induces apoptosis of tumour cells in SCID mice models. This compound has the potential to inhibit the growth of HCC cell-derived tumours in vivo.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23869022/ [2] https://pubmed.ncbi.nlm.nih.gov/12237314/ [3] https://pubmed.ncbi.nlm.nih.gov/25333816/

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