Dimethylcurcumin

SKU: orb1296125

Description

Dimethylcurcumin (ASC-J9) is a small molecule that enhances androgen receptor degradation. It has been shown in research to inhibit the proliferation and invasion of castration-resistant prostate cancer cells in both in vitro and in vivo models, making it a compound of interest for oncology studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 52328-98-0
• MW: 396.43
• Purity: 98.96% (May vary between batches)
• Formula: C₂₃H₂₄O₆
• SMILES: COc1ccc(\C=C\C(\O)=C\C(=O)\C=C\c2ccc(OC)c(OC)c2)cc1OC
• Target: Androgen Receptor
• Solubility: DMSO:48 mg/mL (121.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.05 mM);H2O:Insoluble

Bioactivity

• In Vivo:
  Dimethylcurcumin (75 mg/kg, i.p.) degrades both fAR and AR3 in the xenografted tumors in vivo and ASC-J9-treated tumors have significantly decreased Ki67-positive cells . Dimethylcurcumin (50 mg/kg every 48 h, i.p.) substantially ameliorates the SBMA symptoms in AR-97Q mice and ameliorates neuromuscular pathological findings . ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen .
• In Vitro:
  Dimethylcurcumin is able to degrade fAR and AR3 in a dose-dependent manner in various human PCa cells. Dimethylcurcumin can also effectively suppress AR-targeted genes in CWR22Rv1-fARKD cells. Dimethylcurcumin (5 or 10 μM) significantly suppresses the DHT-induced cell growth in all three PCa cell lines. Dimethylcurcumin suppresses AR-targeted genes and cell growth by the degradation of fAR and ectopic AR3 in C81 and C4-2 cells . ASC-J9 reduces the AR aggregated AR-112Q in cells. Dimethylcurcumin suppresses the aggregation of AR-112Q in SBMA PC12/AR-112Q cells .
• Cell Research:
  For the cell survival assay, the PC12/AR-112Q and PC12/AR-10Q cells are cultured as described previously and incubated cells in the presence of 10 μg/mL doxycycline for 24 h. Then the cells are treated with a vehicle, 5 μM Dimethylcurcumin or 10 μM Dimethylcurcumin, along with 1 nM DHT, and determined cell viability using Trypan blue staining at specific time intervals .
• Animal Research:
  CWR22Rv1 cells (1×10^6 cells per site) are injected into both anterior prostates of the castrated nude mice after 2 weeks of implantation. The mice were randomly divided into two groups (four mice/eight tumors each group) and either receive 75 mg/kg Dimethylcurcumin intraperitoneal injection or vehicle control every other day. After 4 weeks of treatment, all mice are killed to examine the tumor growth. Body weights and mice activity are measured weekly .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ASC-J9, AndrogenReceptor, Androgen Receptor, Dimethylcurcumin, Inhibitor, GO-Y 025, GO-Y025, GO-Y-025, inhibit

Compound Identifiers

PubChem CID

6477182