HO-3867
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
HO-3867是一种新的姜黄素类似物,是STAT3的选择性抑制剂.[1]
STAT3(信号转导和转录激活子3)属于STAT蛋白家族.STAT3介导用于多种细胞功能的各种基因的表达,包括细胞生长\分裂和凋亡.
HO-3867可选择性阻断STAT3磷酸化\转录和DNA结合,而不抑制其他STAT蛋白.该物质可在卵巢癌细胞中激活细胞凋亡,对健康细胞有最低毒性.[2]HO-3867也可显著抑制血清刺激的SMC增殖,并可提高SMC中磷酸化的和总的PTEN水平.[3]HO-3867可通过诱导细胞周期停滞和细胞凋亡,降低子宫内膜癌细胞中高水平的pSTAT3 Ser727.[4]
在小鼠肿瘤异种移植物中,HO-3867可抑制肿瘤生长而不引起毒性副作用,该物质也可阻断PSTAT3/JAK1,并可提高凋亡标志物剪切的Caspase 3/PARP.[2][5]在大鼠颈动脉受伤后,HO-3867可抑制内膜增生,并能上调PTEN表达.[3]
参考文献：
[1] Tierney BJ, McCann GA, Cohn DE, Eisenhauer E, Sudhakar M, Kuppusamy P, Hideg K, Selvendiran K. HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Cancer Biol Ther. 2012 Jul;13(9):766-75.
[2] Rath KS, Naidu SK, Lata P, Bid HK, Rivera BK, McCann GA, Tierney BJ, Elnaggar AC, Bravo V, Leone G, Houghton P, Hideg K, Kuppusamy P, Cohn DE, Selvendiran K.
HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27.
[3] Selvendiran K, Kuppusamy ML, Bratasz A, Tong L, Rivera BK, Rink C, Sen CK, Kálai T, Hideg K, Kuppusamy P. Inhibition of vascular smooth-muscle cell proliferation and arterial restenosis by HO-3867, a novel synthetic curcuminoid, through up-regulation of PTEN expression. J Pharmacol Exp Ther. 2009 Jun;329(3):959-66.
[4] Tierney BJ, McCann GA, Naidu S, Rath KS, Saini U, Wanner R, Kuppusamy P,Suarez A, Goodfellow PJ, Cohn DE, Selvendiran K. Aberrantly activated pSTAT3-Ser727 in human endometrial cancer is suppressed by HO-3867, a novel STAT3 inhibitor. Gynecol Oncol. 2014 Oct;135(1):133-41.
[5] Selvendiran K, Tong L, Bratasz A, Kuppusamy ML, Ahmed S, Ravi Y, Trigg NJ, Rivera BK, Kálai T, Hideg K, Kuppusamy P. Anticancer efficacy of a difluorodiarylidenyl piperidone (HO-3867) in human ovarian cancer cells and tumor xenografts. Mol Cancer Ther. 2010 May;9(5):1169-79.
- 1. Junwei Hou, Rongce Zhao, et al. "PD-L1-mediated gasdermin C expression switches apoptosis to pyroptosis in cancer cells and facilitates tumour necrosis." Nature Cell Biology (2020). PMID:32929201
- 2. Tao X, Zuo Q, et al. "Argininosuccinate synthase 1 suppresses cancer cell invasion by inhibiting STAT3 pathway in hepatocellular carcinoma." Acta Biochim Biophys Sin (Shanghai). 2019 Mar 1;51(3):263-276. PMID:30883650
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 464.55 |
| Cas No. | 1172133-28-6 |
| Formula | C28H30F2N2O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥18.15 mg/mL in DMSO |
| Chemical Name | (3E,5E)-3,5-bis(4-fluorobenzylidene)-1-((1-hydroxy-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)methyl)piperidin-4-one |
| SDF | Download SDF |
| Canonical SMILES | O=C(/C(CN(CC1=CC(C)(C)N(O[H])C1(C)C)C/2)=C/C3=CC=C(F)C=C3)C2=C\C4=CC=C(F)C=C4 |
| 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]: | |
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细胞系 |
A2780人上皮卵巢癌细胞系，卵巢癌细胞系SKOV3、OVCAR3、A2780R和OV4 |
|
溶解方法 |
可溶于DMSO。若获取更高浓度的溶液，可在37℃下孵育10分钟，随后在超声波浴中摇匀。-20℃以下可储存数月。 |
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反应条件 |
10 μmol/L，20 μmol/L，24 h |
|
应用 |
HO-3867对A2780和其他卵巢癌细胞系具有细胞毒性。HO-3867（20 μmol/L）诱导A2780细胞G2/M细胞周期停滞。HO-3867诱导A2780细胞凋亡。HO-3867诱导凋亡并抑制人卵巢癌细胞株JAK/STAT3信号转导。 |
| 动物实验 [1,2]: | |
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动物模型 |
卵巢癌肿瘤异种移植小鼠模型 |
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给药剂量 |
25、50和100 ppm，口服 |
|
应用 |
在卵巢癌肿瘤异种移植小鼠中，HO-3867抑制小鼠异种移植肿瘤的生长。在体内，HO-3867抑制pSTAT3并下调STAT3靶蛋白。口服HO-3867（100 ppm）通过降低大鼠肺中的氧化应激和增加PTEN表达来减弱左心衰竭引起的肺动脉高压。 |
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注意事项 |
由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。 |
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References: [1]. Selvendiran K, Tong L, Bratasz A, et al. Anticancer efficacy of a difluorodiarylidenyl piperidone (HO-3867) in human ovarian cancer cells and tumor xenografts[J]. Molecular cancer therapeutics, 2010, 9(5): 1169-1179. [2]. Ravi Y, Selvendiran K, Naidu S K, et al. Pulmonary hypertension secondary to left-heart failure involves peroxynitrite-induced downregulation of PTEN in the lung[J]. Hypertension, 2013: HYPERTENSIONAHA. 111.00514. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
