BV6
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.
BV6是一种选择性的IAP家族抑制剂,在H460细胞中的IC50值为7.2 μM [1]。
IAP(凋亡抑制子)是由8个成员组成的蛋白家族,作为程序性细胞死亡的内源性抑制子。截至目前,已发现5个以上的人IAPs,包括XIAP、c-IAP1、c-IAP-2、NAIP、Livin和Survivin。据报道,IAPs的过表达可以保护细胞抵抗促凋亡刺激,表明IAPs在促进癌细胞存活方面具有至关重要的作用 [2, 3]。
BV6是IAP家族的抑制剂,通常用作佐剂,增加癌细胞对放疗或化疗的敏感性。在H460 非小细胞肺癌(NSCLC)细胞中,BV6预处理增加细胞对放疗的敏感性,通过减少cIAP1和XIAP的表达,以时间和剂量依赖的方式增加细胞凋亡。在白血病THP-1细胞中,BV6预处理增加CIK细胞的杀伤能力,在实体恶性肿瘤RH30细胞中也得到了同样的结果 [4]。
在从供体小鼠子宫组织获得移植腹腔的BALB / c小鼠模型中,腹腔注射BV6通过抑制IAPs的表达,从而抑制子宫内膜异位症的发展和细胞增殖活性 [5]。
参考文献:
[1]. Li, W., et al., BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol, 2011. 6(11): p. 1801-9.
[2]. Altieri, D.C., Survivin - The inconvenient IAP. Semin Cell Dev Biol, 2015.
[3]. Fulda, S., Smac mimetics as IAP antagonists. Semin Cell Dev Biol, 2014.
[4]. Rettinger, E., et al., SMAC Mimetic BV6 Enables Sensitization of Resistant Tumor Cells but also Affects Cytokine-Induced Killer (CIK) Cells: A Potential Challenge for Combination Therapy. Front Pediatr, 2014. 2: p. 75.
[5]. Uegaki, T., et al., Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod, 2015. 30(1): p. 149-58.
- 1. Yugo Fujita, Toshiyuki Yano, et al. "Enhanced nuclear localization of phosphorylated MLKL predicts adverse events in patients with dilated cardiomyopathy." ESC Heart Fail. 2022 Oct;9(5):3435-3451. PMID: 35851586
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- 8. Lei W, Duan R, et al. "The IAP Antagonist SM-164 Eliminates Triple-Negative Breast Cancer Metastasis to Bone and Lung in Mice." Sci Rep. 2020;10(1):7004. PMID:32332865
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 1205.57 |
Cas No. | 1001600-56-1 |
Formula | C70H96N10O8 |
Solubility | ≥60.28 mg/mL in DMSO; insoluble in H2O; ≥12.6 mg/mL in EtOH with ultrasonic |
Chemical Name | (S,S,2S,2'S)-N,N'-((2S,2'S)-(hexane-1,6-diylbis(azanediyl))bis(3-oxo-1,1-diphenylpropane-3,2-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide) |
SDF | Download SDF |
Canonical SMILES | O=C(CCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)CO=C(NCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)C(C3=CC=CC=C3)C4=CC=CC=C4)=O)[C@@H](NC([C@H]5N(C([C@H](C6CCCCC6)NC([C@H](C)NC)=O)=O)CCC5)=O)C(C7=CC= |
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 |
HCC193和H460非小细胞肺癌(NSCLC)细胞系。 |
制备方法 |
溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37°C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°C可放置数月。 |
反应条件 |
37°C |
实验结果 |
BV6以时间和剂量依赖的方式降低HCC193和H460细胞系中cIAP1和XIAP的表达。在HCC193和H460细胞系中,BV6诱导细胞凋亡。此外,BV6显著促进HCC193和H460肺癌细胞系的放射敏感性。 |
动物实验: [2] | |
动物模型 |
小鼠子宫内膜异位症模型 |
给药剂量 |
腹腔注射,每周注射两次BV6(10 mg/kg)。 |
实验结果 |
BV6处理4周减弱IAP表达的强度,与对照组相比降低病变的总数、平均重量和表面积。此外,BV6减少子宫内膜腺上皮或基质中Ki67阳性细胞的百分比。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: 1. Li W, Li B, Giacalone NJ, Torossian A et al. BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol. 2011 Nov;6(11):1801-9. 2. Uegaki T, Taniguchi F, Nakamura K et al. Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod. 2015 Jan;30(1):149-58. |
描述 | BV6(小分子Smac模拟物)是IAP蛋白的拮抗剂。 | |||||
靶点 | ||||||
IC50 |
质量控制和MSDS
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