1. NF-κB
    Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
  2. NF-κB
    HSP
    Eukaryotic Initiation Factor (eIF)
  3. Rocaglamide

Rocaglamide (Synonyms: Rocaglamide A; Roc-A)

Cat. No.: HY-19356 Purity: 99.34%
Handling Instructions

Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat 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

Rocaglamide Chemical Structure

CAS No. : 84573-16-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 868 In-stock
Estimated Time of Arrival: December 31
200 μg USD 119 In-stock
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1 mg USD 228 In-stock
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5 mg USD 780 In-stock
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10 mg USD 1200 In-stock
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25 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat 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[1][2][3].

IC50 & Target

HSF1

50 nM (IC50)

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].

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].

Molecular Weight

505.56

Formula

C₂₉H₃₁NO₇

CAS No.

84573-16-0

SMILES

O1C2=CC(OC)=CC(OC)=C2[[email protected]]2(O)[[email protected]](O)[[email protected]](C(N(C)C)=O)[[email protected]@H](C3=CC=CC=C3)[[email protected]]12C1=CC=C(OC)C=C1 |&1:11,13,15,21,28,r|

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (296.70 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are provided by MCE.
References
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
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KeyWords:

Rocaglamide | Rocaglamide A | Roc-A | NF-κB | HSP | Eukaryotic Initiation Factor (eIF) | Nuclear factor-κB | Nuclear factor-kappaB | Heat shock proteins | Inhibitor | inhibitor | inhibit

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Product name:
Rocaglamide
Cat. No.:
HY-19356
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