ASC-J9 | GO-Y025 | Dimethylcurcumin | CAS#52328-98-0 | AR degradation enhancer

MedKoo Cat#: 407256 | Name: ASC-J9

Description:

WARNING: This product is for research use only, not for human or veterinary use.

ASC-J9, also known as GO-Y025 and Dimethylcurcumin, is an AR degradation enhancer ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors. ASC-J9 suppresses renal cell carcinoma progression by targeting an androgen receptor-dependent HIF2α/VEGF signaling pathway.ASC-J9 treatment enhanced BCG efficacy to suppress bladder cancer cell proliferation via increasing the recruitment of monocytes/macrophages that involved the promotion of BCG attachment/internalization to the bladder cancer cells through increased integrin-α5β1 expression and IL6 release.

Chemical Structure

ASC-J9

CAS#52328-98-0

Theoretical Analysis

MedKoo Cat#: 407256

Name: ASC-J9

CAS#: 52328-98-0

Chemical Formula: C23H24O6

Exact Mass: 396.1573

Molecular Weight: 396.44

Elemental Analysis: C, 69.68; H, 6.10; O, 24.21

Price and Availability

Size	Price	Availability
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks
200mg	USD 2,050.00	2 Weeks

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Synonym

ASC-J9; ASC J9; GO-Y025; GO-Y 025; GO Y025; Dimethylcurcumin.

IUPAC/Chemical Name

(1E,4Z,6E)-1,7-bis(3,4-dimethoxyphenyl)-5-hydroxyhepta-1,4,6-trien-3-one

InChi Key

ZMGUKFHHNQMKJI-CIOHCNBKSA-N

InChi Code

InChI=1S/C23H24O6/c1-26-20-11-7-16(13-22(20)28-3)5-9-18(24)15-19(25)10-6-17-8-12-21(27-2)23(14-17)29-4/h5-15,24H,1-4H3/b9-5+,10-6+,18-15-

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer.

In vitro activity:

The results revealed that among 195 mapped genes, 105 genes are only increased by ASC-J9®, and not Enz and AR-shRNA, with 23.8% of these ASC-J9® elevated genes have biological regulation (Fig. 1b). Results from GO analysis further revealed that among these ASC-J9® elevated genes, only 11 genes, including ATF3, are responsible for the tumor suppression (Fig. 1b and c). Importantly, results from qRT-PCR assay further confirmed that only ASC-J9®, not Enz or AR-shRNA, could increase ATF3 expression (Fig. 1e). Reference: J Exp Clin Cancer Res. 2021; 40: 3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7780640/

In vivo activity:

When the tumors reached over 200 mm3, the mice were randomized into different treatment groups and then i.p. injected with vehicle control, ASC-J9® (50 mg/kg body weight/3 times per week), Cisplatin (2.5 mg/kg body weight once per week), or the same doses of ASC-J9® combined with Cisplatin for a total of 4 weeks (see the treatment scheme in Additional file 1: Figure S1). The tumor sizes were measured every 3 days for 4 weeks before sacrifice. As shown in Fig. 5a, ASC-J9® or Cisplatin treatment effectively reduced the growth rate of all xenografted tumors compared with control, and Cisplatin combined with ASC-J9® treatment led to the best suppressive effects on xenografted BCa tumor growth. Reference: J Exp Clin Cancer Res. 2019; 38: 275. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6592003/

	Solvent	mg/mL	mM
Solubility
	DMSO	44.7	112.68
	DMF	10.0	25.22
	DMF:PBS (pH 7.2) (1:2)	0.3	0.76
	Ethanol	0.3	0.63

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 396.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Tian H, Chou FJ, Tian J, Zhang Y, You B, Huang CP, Yeh S, Niu Y, Chang C. ASC-J9® suppresses prostate cancer cell proliferation and invasion via altering the ATF3-PTK2 signaling. J Exp Clin Cancer Res. 2021 Jan 4;40(1):3. doi: 10.1186/s13046-020-01760-2. PMID: 33390173; PMCID: PMC7780640. 2. Cheng MA, Chou FJ, Wang K, Yang R, Ding J, Zhang Q, Li G, Yeh S, Xu D, Chang C. Androgen receptor (AR) degradation enhancer ASC-J9® in an FDA-approved formulated solution suppresses castration resistant prostate cancer cell growth. Cancer Lett. 2018 Mar 28;417:182-191. doi: 10.1016/j.canlet.2017.11.038. Epub 2018 Jan 17. PMID: 29203251. 3. Huang CP, Chen J, Chen CC, Liu G, Zhang Y, Messing E, Yeh S, Chang C. ASC-J9® increases the bladder cancer chemotherapy efficacy via altering the androgen receptor (AR) and NF-κB survival signals. J Exp Clin Cancer Res. 2019 Jun 24;38(1):275. doi: 10.1186/s13046-019-1258-0. PMID: 31234917; PMCID: PMC6592003. 4. Lin W, Luo J, Sun Y, Lin C, Li G, Niu Y, Chang C. ASC-J9® suppresses prostate cancer cell invasion via altering the sumoylation-phosphorylation of STAT3. Cancer Lett. 2018 Jul 1;425:21-30. doi: 10.1016/j.canlet.2018.02.007. Epub 2018 Feb 6. PMID: 29425687.

In vitro protocol:

In vivo protocol:

1. Huang CP, Chen J, Chen CC, Liu G, Zhang Y, Messing E, Yeh S, Chang C. ASC-J9® increases the bladder cancer chemotherapy efficacy via altering the androgen receptor (AR) and NF-κB survival signals. J Exp Clin Cancer Res. 2019 Jun 24;38(1):275. doi: 10.1186/s13046-019-1258-0. PMID: 31234917; PMCID: PMC6592003. 2. Lin W, Luo J, Sun Y, Lin C, Li G, Niu Y, Chang C. ASC-J9® suppresses prostate cancer cell invasion via altering the sumoylation-phosphorylation of STAT3. Cancer Lett. 2018 Jul 1;425:21-30. doi: 10.1016/j.canlet.2018.02.007. Epub 2018 Feb 6. PMID: 29425687.

1: Shang Z, Li Y, Zhang M, Tian J, Han R, Shyr CR, Messing E, Yeh S, Niu Y, Chang C. Antiandrogen Therapy with Hydroxyflutamide or Androgen Receptor Degradation Enhancer ASC-J9 Enhances BCG Efficacy to Better Suppress Bladder Cancer Progression. Mol Cancer Ther. 2015 Nov;14(11):2586-94. doi: 10.1158/1535-7163.MCT-14-1055-T. Epub 2015 Aug 11. PubMed PMID: 26264279; PubMed Central PMCID: PMC4704455. 2: Yamashita S, Arai Y. [ASC-J9 for castration-resistant prostate cancer]. Nihon Rinsho. 2014 Dec;72(12):2126-9. Japanese. PubMed PMID: 25518345. 3: Verderio P, Pandolfi L, Mazzucchelli S, Marinozzi MR, Vanna R, Gramatica F, Corsi F, Colombo M, Morasso C, Prosperi D. Antiproliferative effect of ASC-J9 delivered by PLGA nanoparticles against estrogen-dependent breast cancer cells. Mol Pharm. 2014 Aug 4;11(8):2864-75. doi: 10.1021/mp500222k. Epub 2014 Jul 18. PubMed PMID: 24945469. 4: He D, Li L, Zhu G, Liang L, Guan Z, Chang L, Chen Y, Yeh S, Chang C. ASC-J9 suppresses renal cell carcinoma progression by targeting an androgen receptor-dependent HIF2α/VEGF signaling pathway. Cancer Res. 2014 Aug 15;74(16):4420-30. doi: 10.1158/0008-5472.CAN-13-2681. Epub 2014 Jun 12. PubMed PMID: 24924778. 5: Izumi K, Chang C. Targeting inflammatory cytokines-androgen receptor (AR) signaling with ASC-J9(®) to better battle prostate cancer progression. Oncoimmunology. 2013 Dec 1;2(12):e26853. Epub 2013 Oct 22. PubMed PMID: 24498558; PubMed Central PMCID: PMC3902114. 6: Soh SF, Huang CK, Lee SO, Xu D, Yeh S, Li J, Yong EL, Gong Y, Chang C. Determination of androgen receptor degradation enhancer ASC-J9(®) in mouse sera and organs with liquid chromatography tandem mass spectrometry. J Pharm Biomed Anal. 2014 Jan;88:117-22. doi: 10.1016/j.jpba.2013.08.020. Epub 2013 Aug 27. PubMed PMID: 24042123; PubMed Central PMCID: PMC3856572. 7: Lin TH, Izumi K, Lee SO, Lin WJ, Yeh S, Chang C. Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling. Cell Death Dis. 2013 Aug 8;4:e764. doi: 10.1038/cddis.2013.270. PubMed PMID: 23928703; PubMed Central PMCID: PMC3763432. 8: Lin TH, Lee SO, Niu Y, Xu D, Liang L, Li L, Yeh SD, Fujimoto N, Yeh S, Chang C. Differential androgen deprivation therapies with anti-androgens casodex/bicalutamide or MDV3100/Enzalutamide versus anti-androgen receptor ASC-J9(R) Lead to promotion versus suppression of prostate cancer metastasis. J Biol Chem. 2013 Jul 5;288(27):19359-69. doi: 10.1074/jbc.M113.477216. Epub 2013 May 16. PubMed PMID: 23687298; PubMed Central PMCID: PMC3707641. 9: Lai KP, Huang CK, Chang YJ, Chung CY, Yamashita S, Li L, Lee SO, Yeh S, Chang C. New therapeutic approach to suppress castration-resistant prostate cancer using ASC-J9 via targeting androgen receptor in selective prostate cells. Am J Pathol. 2013 Feb;182(2):460-73. doi: 10.1016/j.ajpath.2012.10.029. Epub 2012 Dec 4. PubMed PMID: 23219429; PubMed Central PMCID: PMC3562731. 10: Yamashita S, Lai KP, Chuang KL, Xu D, Miyamoto H, Tochigi T, Pang ST, Li L, Arai Y, Kung HJ, Yeh S, Chang C. 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. PubMed PMID: 22355276; PubMed Central PMCID: PMC3281944. 11: Yang Z, Chang YJ, Yu IC, Yeh S, Wu CC, Miyamoto H, Merry DE, Sobue G, Chen LM, Chang SS, Chang C. ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor. Nat Med. 2007 Mar;13(3):348-53. Epub 2007 Mar 4. PubMed PMID: 17334372.