Art. -Nr.: HY-15194

Dimethylcurcumin

(Synonyms: ASC-J9; GO-Y025)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

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

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Reinheit: 98.01%
CAS. Nr.: 52328-98-0
Formel: C₂₃H₂₄O₆
Molecular Weight:396.43

Speicherung:

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

Dimethylcurcumin Chemical Structure

CAS. Nr.: 52328-98-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	5.8 μM Compound: 3	Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay	[PMID: 21070043]
A549	IC₅₀	>40 μM Compound: 3	Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method	[PMID: 21070043]
HCT-116	GI₅₀	2 μM Compound: GO-Y025	Growth inhibition of human HCT116 cells after 48 hrs by MTS assay Growth inhibition of human HCT116 cells after 48 hrs by MTS assay	[PMID: 20060305]
HEK293	EC₅₀	8.3 μM Compound: 1b	Inhibition of Wnt3A/beta-catenin signaling in HEK293 cells after 24 hrs by firefly/renilla dual luciferase reporter gene assay Inhibition of Wnt3A/beta-catenin signaling in HEK293 cells after 24 hrs by firefly/renilla dual luciferase reporter gene assay	[PMID: 24275249]
KB	CC₅₀	2 μM Compound: 11a	Compound concentration required to reduce the exponential growth of KB cells by 50% Compound concentration required to reduce the exponential growth of KB cells by 50%	[PMID: 9767632]
LNCaP	IC₅₀	1.3 μM Compound: 71, JC-9, ASC-J9	Cytotoxicity against human LNCAP cells after 2 days Cytotoxicity against human LNCAP cells after 2 days	[PMID: 20187635]
LNCaP	IC₅₀	1.3 μM Compound: 2, DMC	Cytotoxicity against human LNCaP cell line Cytotoxicity against human LNCaP cell line	[PMID: 16789753]
LNCaP	IC₅₀	15.3 μM Compound: 21	Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	[PMID: 22672984]
LNCaP	IC₅₀	3.9 μM Compound: 6	Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay Antiproliferative activity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 19249204]
MCF-10A	IC₅₀	31.5 μM Compound: 6	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 19249204]
MCF7	IC₅₀	5.4 μM Compound: 6	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 19249204]
MDA-MB-231	IC₅₀	4.9 μM Compound: 6	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 19249204]
MT4	CC₅₀	4.1 μM Compound: 11a	Compound concentration required to reduce the exponential growth of MT-4 cells by 50% Compound concentration required to reduce the exponential growth of MT-4 cells by 50%	[PMID: 9767632]
PC-3	IC₅₀	1.1 μM Compound: 71, JC-9, ASC-J9	Cytotoxicity against human PC3 cells after 2 days Cytotoxicity against human PC3 cells after 2 days	[PMID: 20187635]
PC-3	IC₅₀	1.1 μM Compound: 2, DMC	Cytotoxicity against human PC3 cell line Cytotoxicity against human PC3 cell line	[PMID: 16789753]
PC-3	IC₅₀	23.7 μM Compound: 21	Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay	[PMID: 22672984]
PC-3	IC₅₀	5.9 μM Compound: 6	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 19249204]
SK-OV-3	IC₅₀	3.51 μM Compound: 15	Cytotoxicity against human SKOV3 Cells after 48 hrs by Cell Titer Blue assay Cytotoxicity against human SKOV3 Cells after 48 hrs by Cell Titer Blue assay	[PMID: 31129455]

In Vitro

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].

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

In Vivo

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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 52328-98-0
Appearance Solid
Molecular Weight 396.43
Formel C₂₃H₂₄O₆
Color Yellow to orange
SMILES

O=C(/C=C(O)/C=C/C1=CC=C(OC)C(OC)=C1)/C=C/C2=CC=C(OC)C(OC)=C2
Synonyms

ASC-J9; GO-Y025
Structure Classification
- Phenylpropanoids
- Simple Phenylpropanols
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (14)

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Journal Impact Factor

Clin Transl Med

Both SUMOylation and ubiquitination of TFE3 fusion protein regulated by androgen receptor are the potential target in the therapy of Xp11.2 translocation renal cell carcinoma. [Abstract]

2022 Apr;12(4):e797. PMID: 35452181
Mol Cancer Ther

The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide. [Abstract]

2016 Jul;15(7):1702-12. PMID: 27196756
Biochem Pharmacol

Testosterone regulates 3T3-L1 pre-adipocyte differentiation and epididymal fat accumulation in mice through modulating macrophage polarization. [Abstract]

2017 Sep 15:140:73-88. PMID: 28642037

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2017 Sep 15:140:73-88. [Abstract]

Androgen receptors levels in RAW264.7 cells treated with ASC-J9. Cells are treated with or without ASC-J9 for 30 min or 12 h and cells lysate is examined by western blotting using antibodies for the Androgen Receptor and GAPDH.
EXCLI J

2019 Jan 24;18:21-29.
Biol Sex Differ

Neuroprotective and neurotoxic outcomes of androgens and estrogens in an oxidative stress environment. [Abstract]

2020 Mar 29;11(1):12. PMID: 32223745
J Ovarian Res

Nanog interaction with the androgen receptor signaling axis induce ovarian cancer stem cell regulation: studies based on the CRISPR/Cas9 system. [Abstract]

2018 May 2;11(1):36. PMID: 29716628

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: J Ovarian Res. 2018 May 2;11(1):36. [Abstract]

Oct4 and Sox2 expression in the GFP (+) cells clearly increased under DHT treatment compared with ASC-J9 treatment based on western blot analysis, which is also consistent with the Nanog expression trend.
Transl Oncol

Breaking androgen receptor addiction of prostate cancer by targeting different functional domains in the treatment of advanced disease. [Abstract]

2021 Aug;14(8):101115. PMID: 33993099
Lab Invest

Androgen receptor transcriptionally inhibits programmed death ligand-1 (PD-L1) expression and influences immune escape in bladder cancer. [Abstract]

2023 Jul;103(7):100148. PMID: 37059268
Endocrinology

NADPH Oxidase Mediates Membrane Androgen Receptor-Induced Neurodegeneration. [Abstract]

2019 Apr 1;160(4):947-963. PMID: 30811529
J Steroid Biochem Mol Biol

(-)-Epicatechin acts as a potent agonist of the membrane androgen receptor, ZIP9 (SLC39A9), to promote apoptosis of breast and prostate cancer cells. [Abstract]

2021 Jul:211:105906. PMID: 33989703
Biochem Biophys Res Commun

Androgen receptor regulates cardiac fibrosis in mice with experimental autoimmune myocarditis by increasing microRNA-125b expression. [Abstract]

2018 Nov 17;506(1):130-136. PMID: 30340830

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Nov 17;506(1):130-136. [Abstract]

The protein expression level of AR in EAM mice with/without ASC-J9 treatment is analysed.

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Nov 17;506(1):130-136. [Abstract]

Treatment with ASC-J9 in the presence of TGF-b decreases the mRNA expression of collagen I and a-SMA.
Biochem Biophys Res Commun

Targeting androgen receptor with ASC-J9 attenuates cardiac injury and dysfunction in experimental autoimmune myocarditis by reducing M1-like macrophage. [Abstract]

2017 Apr 15;485(4):746-752. PMID: 28246012

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Apr 15;485(4):746-752. [Abstract]

ASC-J9 inhibits M1 polarization of Raw264.7 cells. (A) Western blotting and analysis of iNOS in Raw264.7 cells stimulated with LPS in each group. (B) Western blotting and analysis of SOCS1 and p-STAT5 expression in Raw264.7 cells stimulated with LPS in each group.
Oncotarget

Androgen/androgen receptor axis maintains and promotes cancer cell stemness through direct activation of Nanog transcription in hepatocellular carcinoma. [Abstract]

2016 Jun 14;7(24):36814-36828. PMID: 27167111

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 14;7(24):36814-36828. [Abstract]

Protein levels of AR and NANOG expression is measured in Nanog^Pos and Nanog^Neg cells from T1224+1 and Huh7+7 after treatment with DHT and with or without ASC-J9 for 24h. The addition of ASC-J9 attenuates the DHT effect and reduces the expression of AR and Nanog in both groups.
Tumour Biol

Gabarapl1 mediates androgen-regulated autophagy in prostate cancer. [Abstract]

2015 Nov;36(11):8727-33. PMID: 26050226

Dimethylcurcumin purchased from MedChemExpress. Usage Cited in: Tumour Biol. 2015 Nov;36(11):8727-33. [Abstract]

Application of ASC-J9 (an AR degradation enhancer) to 22Rv1 cell line also represses androgen-induced Gabarapl1 upregulation.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (126.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5225 mL

12.6126 mL

25.2251 mL

5 mM

0.5045 mL

2.5225 mL

5.0450 mL

10 mM

0.2523 mL

1.2613 mL

2.5225 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

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.

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

Animal Administration^[1]

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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5225 mL	12.6126 mL	25.2251 mL	63.0628 mL
	5 mM	0.5045 mL	2.5225 mL	5.0450 mL	12.6126 mL
	10 mM	0.2523 mL	1.2613 mL	2.5225 mL	6.3063 mL
	15 mM	0.1682 mL	0.8408 mL	1.6817 mL	4.2042 mL
	20 mM	0.1261 mL	0.6306 mL	1.2613 mL	3.1531 mL
	25 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5225 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1021 mL
	40 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5766 mL
	50 mM	0.0505 mL	0.2523 mL	0.5045 mL	1.2613 mL
	60 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0510 mL
	80 mM	0.0315 mL	0.1577 mL	0.3153 mL	0.7883 mL
	100 mM	0.0252 mL	0.1261 mL	0.2523 mL	0.6306 mL

Keywords

Dimethylcurcumin

14 Cited Publications

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Dimethylcurcumin

AZD3514

Bavdegalutamide

Vosilasarm

MK-0773

3,3'-Diindolylmethane

GSK-2881078

MG-132

RU 58841

BMS-564929

GTx-007

LY2452473

Curcumin

Publications Citing Use of MedChemExpress (MCE) Dimethylcurcumin

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dimethylcurcumin

AZD3514

Bavdegalutamide

Vosilasarm

MK-0773

3,3'-Diindolylmethane

GSK-2881078

MG-132

RU 58841

BMS-564929

GTx-007

LY2452473

Curcumin

Publications Citing Use of MedChemExpress (MCE) Dimethylcurcumin

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dimethylcurcumin Related Classifications

HY-15194 Related Classifications