Apogossypolone (ApoG2)
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.
Apogossypolone是Bcl-2、Mcl-1和Bcl-XL的抑制剂,Ki值分别为35 nM、25 nM和660 nM[1]。
基于MTT的细胞毒性试验表明apogossypolone具有抗癌活性,对PC-3、DU-145(人类前列腺癌细胞系)和MDA-MB-231(人类乳腺癌细胞系)的IC50值为1、2和3 μM。Apogossypolone也可抑制DU-145细胞的集落生成。机理是apogossypolone与Bcl-2结合,阻止其与仅有BH3的促凋亡蛋白的联系,促使促凋亡蛋白参与凋亡响应[2]。
除了前列腺癌和乳腺癌,apogossypolone对滤泡性淋巴瘤也有效。Apogossypolone在WSU-FSCCL细胞系中可通过诱发细胞凋亡,显著抑制细胞生长,72 h时IC50值为109.2 nM[3]。
参考文献:
[1] Zhang XQ, Huang XF, Hu XB, Zhan YH, An QX, Yang SM, Xia AJ, Yi J, Chen R, Mu SJ, Wu DC. Apogossypolone, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces autophagy of PC-3 and LNCaP prostate cancer cells in vitro. Asian J Androl. 2010 Sep;12(5):697-708.
[2] Zhan Y, Jia G, Wu D, Xu Y, Xu L. Design and synthesis of a gossypol derivative with improved antitumor activities. Arch Pharm (Weinheim). 2009 Apr;342(4):223-9.
[3] Arnold AA, Aboukameel A, Chen J, Yang D, Wang S, Al-Katib A, Mohammad RM. Preclinical studies of Apogossypolone: a new nonpeptidic pan small-molecule inhibitor of Bcl-2, Bcl-XL and Mcl-1 proteins in Follicular Small Cleaved Cell Lymphoma model. Mol Cancer. 2008 Feb 14;7:20.
- 1.Lin D, Wang X, et al. "Apogossypolone acts as a metastasis inhibitor via up-regulation of E-cadherin dependent on the GSK-3/AKT complex." Am J Transl Res. 2019 Jan 15;11(1):218-232. PMID:30787981
- 2.Lin D, Li X, et al. "Apogossypolone (ApoG2) induces ROS-dependent apoptosis and reduces invasiveness of PC12 cells in vitro and in vivo." Am J Transl Res. 2017 Sep 15;9(9):3990-4002. eCollection 2017. PMID:28979675
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 490.5 |
Cas No. | 886578-07-0 |
Formula | C28H26O8 |
Solubility | ≥24.55 mg/mL in DMSO; insoluble in H2O; ≥51.2 mg/mL in EtOH with ultrasonic |
Chemical Name | 6,6',7,7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-1,1',4,4'-tetraone |
SDF | Download SDF |
Canonical SMILES | CC1=C(C(C(C2=C3C(C(C)C)=C(O)C(O)=C2)=O)=C(C)C3=O)C(C4=C(C1=O)C(C(C)C)=C(O)C(O)=C4)=O |
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 |
人前列腺癌PC-3和LNCaP细胞系 |
溶解方法 |
在DMSO中的溶解度大于10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
24-96 h,5-20 mg/L |
应用 |
Apogossypolone是一种新型的Bcl-2家族蛋白抑制剂,它以剂量依赖的方式抑制PC-3和LNCaP细胞的生长。用Apogossypolones处理PC-3和LNCaP细胞可诱导自噬,细胞质中出现膜空泡,有酸性自噬泡形成。Apogossypolones处理后两种细胞系的自噬相关蛋白beclin-1和LC3-II表达增加。 |
动物实验[2]: | |
动物模型 |
4周龄的雄性Balb/c nu/nu裸鼠 |
剂量 |
2.5, 5, 10 mg/kg的剂量腹腔给药,每天1次,持续10天 |
应用 |
Apogossypolone能够显著抑制前列腺癌皮下种植体的生长。Apogossypolone可降低肿瘤组织内PCNA和CD31的表达,上调caspases-3和caspase-8的表达,表明Apogossypolone可诱导细胞凋亡,抑制肿瘤增殖和血管生成。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Zhang X Q, Huang X F, Hu X B, et al. Apogossypolone, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces autophagy of PC-3 and LNCaP prostate cancer cells in vitro[J]. Asian journal of andrology, 2010, 12(5): 697. [2]. Xianqing Z, Xiaofeng H, Shijie M, et al. Inhibitory effect of a new gossypol derivative apogossypolone (ApoG2) on xenograft of human prostate cancer cell line PC-3[J]. Journal of Medical Colleges of PLA, 2009, 24(5): 274-282. |
Description | Apogossypolone是一种Bcl-2的非肽类小分子抑制剂。 | |||||
靶点 | Bcl-2 | |||||
IC50 |
质量控制和MSDS
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