Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.

Dimethylcurcumin (ASC-J9) is able to degrade fAR and AR3 in a dose-dependent manner in various human PCa cells. Dimethylcurcumin (ASC-J9) can also effectively suppress AR-targeted genes in CWR22Rv1-fARKD cells. Dimethylcurcumin (ASC-J9) (5 or 10 µM) significantly suppresses the DHT-induced cell growth in all three PCa cell lines. Dimethylcurcumin (ASC-J9) suppresses AR-targeted genes and cell growth by degradation of fAR and ectopic AR3 in C81 and C4-2 cells^[1]. Dimethylcurcumin (ASC-J9) selectively promotes AR degradation by disrupting the interaction between AR and AR coregulators. ASC-J9 reduces the AR aggregated AR-112Q in cells. Dimethylcurcumin (ASC-J9) suppresses the aggregation of AR-112Q in SBMA PC12/AR-112Q cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Dimethylcurcumin (ASC-J9) (75 mg/kg, i.p.) degrades both fAR and AR3 in the xenografted tumors in vivo, and SC-J9-treated tumors has significantly decreased Ki67-positive cells^[1]. Dimethylcurcumin (ASC-J9) (50 mg/kg every 48 h, i.p.) substantially ameliorates the SBMA symptoms in AR-97Q mice, and ameliorates neuromuscular pathological findings. The Dimethylcurcumin (ASC-J9)-treated SBMA mice have relatively normal serum testosterone concentrations^[2]. ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

396.43

C₂₃H₂₄O₆

52328-98-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL (126.13 mM)

* “≥” means soluble, but saturation unknown.

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• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.17 mg/mL (5.47 mM); Clear solution

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  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• [1]. Yamashita S, et al. ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors. Neoplasia. 2012 Jan;14(1):74-83.

  [2]. Yang Z, et al. ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor. Nat Med. 2007 Mar;13(3):348-53.

  [3]. Lee SO, et al. New therapy targeting differential androgen receptor signaling in prostate cancer stem/progenitor vs non-stem/progenitor cells. J Mol Cell Biol. 2012 Jul 24.

  [4]. Ma W, et al. Targeting androgen receptor with ASC-J9 attenuates cardiac injury and dysfunction in experimental autoimmune myocarditis by reducing M1-like macrophage. Biochem Biophys Res Commun. 2017 Apr 15;485(4):746-752. doi: 10.1016/j.bbrc.2017.02.123. Epub 2017 Feb 27.

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 vehicle, 5 μM Dimethylcurcumin (ASC-J9) or 10 μM Dimethylcurcumin (ASC-J9), along with 1 nM DHT, and determined cell viability using Trypan blue staining at specific time intervals.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

CWR22Rv1 cells (1×10⁶ cells per site) are injected into both anterior prostates of castrated nude mouse after 2 weeks of implantation. The mice are randomLy divided into two groups (four mice/eight tumors each group) and either receives 75 mg/kg Dimethylcurcumin (ASC-J9) 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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Yamashita S, et al. ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors. Neoplasia. 2012 Jan;14(1):74-83.

  [2]. Yang Z, et al. ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor. Nat Med. 2007 Mar;13(3):348-53.

  [3]. Lee SO, et al. New therapy targeting differential androgen receptor signaling in prostate cancer stem/progenitor vs non-stem/progenitor cells. J Mol Cell Biol. 2012 Jul 24.

  [4]. Ma W, et al. Targeting androgen receptor with ASC-J9 attenuates cardiac injury and dysfunction in experimental autoimmune myocarditis by reducing M1-like macrophage. Biochem Biophys Res Commun. 2017 Apr 15;485(4):746-752. doi: 10.1016/j.bbrc.2017.02.123. Epub 2017 Feb 27.