ASC-J9
ASC-J9 (CAS 52328-98-0) is a small-molecule degrader targeting androgen receptor (AR). By promoting degradation of full-length AR and splice variants such as AR3/fAR, ASC-J9 inhibits androgen receptor signaling pathways involved in castration-resistant prostate cancer (CRPC) progression and metastatic behavior. ASC-J9 interferes with AR-dependent transcriptional modulation and AR-independent signaling pathways, notably inhibiting STAT3 phosphorylation and CCL2 chemokine secretion, thus reducing macrophage infiltration and prostate cancer invasiveness. Research indicates ASC-J9 may represent an alternative therapeutic strategy for CRPC treatment and metastasis prevention.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 396.43 |
| Cas No. | 52328-98-0 |
| Formula | C23H24O6 |
| Synonyms | GO-Y025; Dimethylcurcumin; ASC J9; GO Y025 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥16.65 mg/mL in DMSO |
| Chemical Name | (1E,4Z,6E)-1,7-bis(3,4-dimethoxyphenyl)-5-hydroxyhepta-1,4,6-trien-3-one |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC(/C=C/C(/C=C(O)/C=C/C2=CC=C(OC)C(OC)=C2)=O)=CC=C1OC |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Human C4-2B/human THP1 cells and mouse TRAMP-C1/mouse RAW264.7 cells. |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
5 μM; 3 days. |
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Applications |
ASC-J9 suppresses macrophage recruitment and suppresses PCa invasion. |
| Animal experiment [1]: | |
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Animal models |
Male 6- to 8-week-old nude mice with orthotopically xenografted 106 TRAMP-C1 cells. |
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Dosage form |
75 mg/kg; i.p. injected three times per week for 3 weeks. |
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Applications |
In mice, ASC-J9 significantly decreases developing distant metastatic tumors in diaphragm and lymph nodes. There are little change in mice body weight among all the mice treated. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Lin TH, Izumi K, Lee SO, et al. 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, 4: e764. |
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| Description | ASC-J9 is an enhancer of androgen receptor degradation. | |||||
| Targets | PC-3 cell proliferation | LNCaP cell proliferation | ||||
| IC50 | 5.9 μM | 3.9 μM | ||||
Quality Control & MSDS
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Chemical structure
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