BIBR 1532
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.
BIBR 1532是端粒酶一个新型的选择性抑制剂,IC50值为93 nM[1]。
据报道,BIBR 1532抑制端粒酶和hTERT的逆转录酶,缩短端粒酶的长度来抑制人类癌细胞增殖[1]。在前-B急性淋巴白血病细胞中,BIBR 1532以浓度依赖的方式抑制c-Myc和hTERT表达来抑制端粒酶活性,高剂量的BIBR 1532可通过提升p73、Bax/Bcl-2和Caspase-3活性而诱导细胞凋亡[2]。在NB4白血病细胞中,可通过c-Myc和hTERT的转录抑制,结合BIBR 1532和三氧化二砷抑制细胞增殖能力和端粒酶活性[3]。
参考文献:
[1]. Damm, K.; Hemmann, U.; Garin-Chesa, P.; Hauel, N.; Kauffman, I.; Priepke, H.; Niestroj, C.; Daiber, C.; Enenkel, B.; Guilliard, B.; Lauritsch, I.; Muller, E.; Pascolo, E.; Sauter, G.; Pantic, M.; Martens, U. M.; Wenz, C.; Linger, J.; Kraut, N.; Rettig, W. J.;Schnapp, A. A highly selective telomerase inhibitor limiting human cancer cell proliferation. EMBO J. 2001, 20, 69586968.
[2]. Bashash D1, Ghaffari SH, Mirzaee R, Alimoghaddam K, Ghavamzadeh A. Telomerase inhibition by non-nucleosidic compound BIBR1532 causes rapid cell death in pre-B acute lymphoblastic leukemia cells. Leuk Lymphoma. 2013 Mar;54[4]:561-8. doi: 10.3109/10428194.2012.704034. Epub 2012 Sep 28.
[3]. Bashash D1, Ghaffari SH, Zaker F, Kazerani M, Hezave K, Hassani S, Rostami M, Alimoghaddam K, Ghavamzadeh A. Anticancer Agents Med Chem. 2013 Sep;13(7):1115-25. BIBR 1532 increases arsenic trioxide-mediated apoptosis in acute promyelocytic leukemia cells: therapeutic potential for APL.
- 1. Qianqian Zhang, Wei Feng, et al. "PPARγ Agonist Pioglitazone Inhibits PDGF-induced Pulmonary Artery Smooth Muscle Cells Proliferation and Migration via Modulating TERT." Biomed Pharmacother. 2022 Aug;152:113233. PMID: 35689861
- 1. Doğan F, Özateş NP, et al. "Investigation of the effect of telomerase inhibitor BIBR1532 on breast cancer and breast cancer stem cells." J Cell Biochem. 2018 Oct 28. PMID: 30368861
- 2. Biray Avci C, Dogan F, et al."Effects of telomerase inhibitor on epigenetic chromatin modification enzymes in malignancies." J Cell Biochem. 2018 Aug 26. PMID: 30145821
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 331.36 |
Cas No. | 321674-73-1 |
Formula | C21H17NO3 |
Solubility | insoluble in H2O; ≥15.65 mg/mL in DMSO; ≥2.36 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid |
SDF | Download SDF |
Canonical SMILES | CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2 |
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。 |
激酶实验 [1]: | |
常规端粒酶活性测定 |
采用内源性端粒酶进行直接的端粒酶活性测定。将10 μL富含端粒酶的提取物与不同浓度的BIBR 1532混合,最终体积为20 μL。将其置于冰上预孵育15分钟后,加入20 μL反应混合物,再将管置于37 °C下开始反应。反应混合物的最终浓度为25mM Tris-Cl (pH 8.3),1mM MgCl2,1 mM EGTA,1mM dATP,1mM dTTP,6.3 μM冷dGTP,15 μCi [α-32P]dGTP (3000 Ci/mmol),1.25 mM亚精胺,10单位的RNasin,5 mM 2-巯基乙醇以及2.5 μM TS引物 (5'-AATCCGTCGAGCAGAGTT)。 |
细胞实验 [2]: | |
细胞系 |
Nalm-6细胞 |
制备方法 |
在DMSO中的溶解度大于15.65 mg/mL。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 |
10、30、60和90 μ M;持续48小时 |
实验结果 |
在Nalm-6细胞中,于30 μM、60 μM和90 μM浓度下,BIBR 1532分别减少了10%、17%和28%的DNA合成率。MTT测定分析结果显示,BIBR 1532呈浓度依赖性地降低Nalm-6细胞代谢活性(30 μM、60 μM和90 μM浓度对应15%、30%和44%的细胞代谢活性降低)。在10 μM和30 μM的剂量下,BIBR 1532部分抑制端粒酶活性,而在较高剂量下,即60 μM和90 μM,BIBR 1532显著抑制端粒酶。 |
References: [1]. Pascolo E, Wenz C, Lingner J, Hauel N, Priepke H, Kauffmann I, Garin-Chesa P, Rettig WJ, Damm K, Schnapp A. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [2]. Bashash D1, Ghaffari SH, Mirzaee R, Alimoghaddam K, Ghavamzadeh A. Telomerase inhibition by non-nucleosidic compound BIBR1532 causes rapid cell death in pre-B acute lymphoblastic leukemia cells. Leuk Lymphoma. 2013 Mar;54[4]:561-8. |
描述 | BIBR 1532是端粒酶的选择性抑制剂,对于人的端粒酶IC50值为93 nM。 | |||||
靶点 | human telomerase | |||||
IC50 | 93 nM |
质量控制和MSDS
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