ASC-J9
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ASC-J9是一种抗肿瘤药物。ASC-J9通过降解全长和剪接变异雄激素受体,从而抑制阉割性前列腺癌的生长。ASC-J9靶向fAR和AR3介导的PCa生长可能代表了新的治疗方法,用于抑制阉割性前列腺癌的生长。ASC-J9通过降解雄激素受体可改善脊髓延髓肌萎缩表型。
雄激素受体(AR)是一种核受体,通过结合细胞质中的雄性激素(睾酮或二氢睾酮)而被激活,然后易位进入细胞核[1]。雄激素与雄激素受体(AR)的结合导致构象变化,从而引起HSP分离,从细胞质运输进入细胞核并进行二聚化。AR二聚体与特异性的DNA序列(HRE)结合,HRE可与核内的其它蛋白结合,导致特异性基因转录的上调或下调[2]。
ASC-J9是AR降解的增强子,抑制巨噬细胞迁移和随后的前列腺癌细胞侵袭。此外,ASC-J9通过两种途径调控pSTAT3-CCL2信号:AR依赖的途径抑制PIAS3的表达和AR不依赖的途径直接抑制STAT3的磷酸化/激活(原位植入TRAMP-C1细胞的小鼠模型)。总之,ASC-J9同时靶向雄激素/ AR信号和PIAS3-pSTAT3-CCL2信号,其单独或联合治疗提供了一种新型更好的治疗策略,用于抑制阉割性前列腺癌的生长和转移[3]。
参考文献:
1. Lu NZ. et al. "International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors". Pharmacol. Rev. 2006, 58 (4): 782–97.
2. Heemers HV, Tindall DJ. "Androgen receptor (AR) coregulators: a diversity of functions converging on and regulating the AR transcriptional complex". Endocr. Rev. 2007, 28 (7): 778–808.
3. Lin TH. 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.
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
人类C4-2B/人类THP1细胞和小鼠TRAMP-C1/小鼠RAW264.7细胞。 |
溶解方法 |
可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
5 μM;3 days |
实验结果 |
ASC-J9抑制巨噬细胞募集并抑制PCa侵袭。 |
动物实验[1]: | |
动物模型 |
原位异种移植106 TRAMP-C1细胞的雄性6至8周龄裸鼠 |
剂量 |
75 mg/kg;腹膜内给药。每周注射三次,持续3周。 |
实验结果 |
在小鼠中,ASC-J9显著减少隔膜和淋巴结中的远端转移性肿瘤的发生。在所有处理的小鼠中小鼠体重几乎没有变化。 |
注意事项 |
请测试室内所有化合物的溶解度,实际溶解度可能与理论值略有不同。这是由实验系统错误引起的,这是正常的。 |
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. |
描述 | ASC-J9是雄激素受体降解的增强子。 | |||||
靶点 | PC-3 cell proliferation | LNCaP cell proliferation | ||||
IC50 | 5.9 μM | 3.9 μM |
质量控制和MSDS
- 批次:
化学结构
![ASC-J9](http://www.apexbt.com/media/diy/images/struct/A3190.png)
相关生物数据
![ASC-J9 ASC-J9](http://www.apexbt.com/media/diy/images/wb/A3190_1.jpg)