Rocaglamide (Synonyms: Roc-A; MG-002)

Name: Rocaglamide
Brand: MedChemExpress
SKU: HY-19356
Rating: 5.0 (23 reviews)

Cat. No.: HY-19356 Purity: 98.76%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC₅₀ of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.

For research use only. We do not sell to patients.

Rocaglamide Chemical Structure

CAS No. : 84573-16-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
500 μg	In-stock	Estimated Time of Arrival: December 31
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Rocaglamide:

Aglafoline In-stock
Didesmethylrocaglamide Get quote

22 Publications Citing Use of MCE Rocaglamide

: Rocaglamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 17;12(1):3720. [Abstract]; The expression of PRDX3 and stem cell markers is decreased upon rocaglamide A (RocA) treatment in a time-dependent and dose-dependent manner.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

eIF4	HSF1 50 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	2.6 μM Compound: Rocaglamide	Inhibition of TNF alpha-induced NF-kappaB (unknown origin) activation in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF alpha-induced NF-kappaB (unknown origin) activation in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 26863083]
HeLa	IC₅₀	0.075 μM Compound: Rocaglamide	Inhibition of NFkappa p65 isolated from nuclear extract of human HeLa cells by ELISA Inhibition of NFkappa p65 isolated from nuclear extract of human HeLa cells by ELISA	[PMID: 21513293]
HeLa	IC₅₀	0.075 μM Compound: Rocaglamide	Inhibition of NFkappa p65 in nuclear extract of human HeLa cells assessed as blockade of NFkappa p65 binding to biotinylated-consesus sequence by ELISA Inhibition of NFkappa p65 in nuclear extract of human HeLa cells assessed as blockade of NFkappa p65 binding to biotinylated-consesus sequence by ELISA	[PMID: 21428375]
HeLa	IC₅₀	0.075 μM Compound: rocaglamide	Inhibition of NFkappa p50 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay Inhibition of NFkappa p50 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay	[PMID: 20384315]
HeLa	IC₅₀	0.1 μM Compound: 7; RocA	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by [35S] methionine incorporation assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by [35S] methionine incorporation assay	[PMID: 33592144]
HeLa	IC₅₀	0.12 μM Compound: Rocaglamide	Inhibition of TNF alpha stimulated NF-KappaB p65 in human HeLa nuclear extract assessed as decrease in NF-KappaB translocation to nucleus measured after 5 hrs by ELISA Inhibition of TNF alpha stimulated NF-KappaB p65 in human HeLa nuclear extract assessed as decrease in NF-KappaB translocation to nucleus measured after 5 hrs by ELISA	[PMID: 31120251]
HeLa	ED₅₀	2 μM Compound: rocaglamide	Inhibition of NF kappaB p50 subunit signaling pathway in human HeLa cells by biotinylated-ELISA Inhibition of NF kappaB p50 subunit signaling pathway in human HeLa cells by biotinylated-ELISA	[PMID: 19422206]
HeLa	IC₅₀	4 μM Compound: rocaglamide	Inhibition of NFkappa p65 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay Inhibition of NFkappa p65 isolated from nuclear extract of human HeLa cells assessed as blockade of binding to biotinylated consesus sequence by chemiluminescence assay	[PMID: 20384315]
MDA-MB-231	IC₅₀	135 nM Compound: (-)-2; (-)-Roc A	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CCGCCG in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CCGCCG in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	20 nM Compound: (-)-2; (-)-Roc A	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	231 nM Compound: (-)-2; (-)-Roc A	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CAACAA in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat CAACAA in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	4.7 nM Compound: (-)-2; (-)-Roc A	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat AGAGAG in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
MDA-MB-231	IC₅₀	47 nM Compound: (-)-2; (-)-Roc A	Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat GGCGGC in 5'- UTR containing luciferase reporter gene assay Inhibition of eIF4A1 in human MDA-MB-231 cells assessed as inhibition of cellular-translation incubated for 4 hrs by specific tandem sequence motif repeat GGCGGC in 5'- UTR containing luciferase reporter gene assay	[PMID: 32470302]
NCI-H929	IC₅₀	3.9 μM Compound: Rocaglamide	Cytotoxicity against human NCI-H929 cells after 48 hrs by MTS assay Cytotoxicity against human NCI-H929 cells after 48 hrs by MTS assay	[PMID: 26863083]

In Vitro

Rocaglamide enhances TRAIL-induced apoptosis in resistant HCC cells. 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. A similar result is obtained by measurement of cell viability using crystal violet staining. Rocaglamide has the potential to sensitize highly chemoresistant HepG2 and Huh-7 cells to TRAIL-based therapy^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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, suggesting that Rocaglamide is generally tolerated well^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

505.56

Formula

C₂₉H₃₁NO₇

CAS No.

84573-16-0

Appearance

Solid

Color

White to off-white

SMILES

O[C@]12[C@](OC3=CC(OC)=CC(OC)=C32)(C4=CC=C(C=C4)OC)[C@H](C5=CC=CC=C5)[C@H]([C@H]1O)C(N(C)C)=O

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (197.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9780 mL	9.8900 mL	19.7800 mL
5 mM	0.3956 mL	1.9780 mL	3.9560 mL
10 mM	0.1978 mL	0.9890 mL	1.9780 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (14.84 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (14.84 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 5% DMSO 95% Saline
Solubility: ≥ 4.76 mg/mL (9.42 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.34%

Select Batch:

Data Sheet (291 KB) SDS (393 KB)

COA (266 KB) HNMR (254 KB) RP-HPLC (326 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. 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 [Content Brief]

[3]. 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. [Content Brief]

Cell Assay ^[2]	HepG2 and Huh-7 cells (1×10⁴/well) are seeded in 96-well plates in complete culture medium and incubated for 24 h. The cells are then exposed to 100 nM Rocaglamide and/or 100 ng/mL TRAIL for 24 h. 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 μL, 0.5 mg/mL in 10% FBS-containing DMEM) is added to each well and the plate is incubated for 2 h at 37°C in a humidified incubator. The solution is then removed from the wells and 200 μL DMSO is added to each well prior to agitation. The absorbance at 570 nm 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 (1×10⁵/mL) are seeded in a 12 well plate for 12 h, and treated with TRAIL (0-100 ng/mL) and/or RocA(1-100 nM) for 12 h. The treated cells are washed with phosphate-buffered saline (PBS), fixed with 4% paraformaldehyde for 15 min, and stained using crystal violet for a further 30 min^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] The Huh-7 cells (3×10⁶), suspended in 100 μL 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 μL 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief] [2]. 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 [Content Brief] [3]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9780 mL	9.8900 mL	19.7800 mL	49.4501 mL
	5 mM	0.3956 mL	1.9780 mL	3.9560 mL	9.8900 mL
	10 mM	0.1978 mL	0.9890 mL	1.9780 mL	4.9450 mL
	15 mM	0.1319 mL	0.6593 mL	1.3187 mL	3.2967 mL
	20 mM	0.0989 mL	0.4945 mL	0.9890 mL	2.4725 mL
	25 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9780 mL
	30 mM	0.0659 mL	0.3297 mL	0.6593 mL	1.6483 mL
	40 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2363 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	60 mM	0.0330 mL	0.1648 mL	0.3297 mL	0.8242 mL
	80 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6181 mL
	100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.4945 mL

Rocaglamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rocaglamide84573-16-0Roc-A MG-002MG002MG 002MG-002NF-κBHSPEukaryotic Initiation Factor (eIF)Nuclear factor-κBNuclear factor-kappaBHeat shock proteinsInhibitorinhibitorinhibit

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Rocaglamide (Synonyms: Roc-A; MG-002)

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Other Forms of Rocaglamide:

Rocaglamide Related Antibodies

22 Publications Citing Use of MCE Rocaglamide

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Protocol

Purity & Documentation

References

Customer Review

Rocaglamide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rocaglamide Related Classifications

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