BRACO 19 trihydrochloride
目录号 : GC50140BRACO 19 trihydrochloride是一种有效的端粒酶/端粒抑制剂，IC50值为115±18nM，可防止端粒酶的加帽和催化作用。
Cas No.:1177798-88-7
Sample solution is provided at 25 µL, 10mM.
BRACO 19 trihydrochloride is a potent telomerase/telomere inhibitor with an IC50 value of 115±18nM, which prevents telomerase capping and catalysis[1]. BRACO 19 trihydrochloride is an acridine compound that acts as a quadruplex (GQ) binding ligand, stabilizing the formation of GQ quadruplexes at 3V telomeric DNA, leading to rapid senescence or selective cell death[2]. BRACO 19 trihydrochloride is a cancer cell proliferation inhibitor[3]. BRACO 19 trihydrochloride has anti-HIV-1 viral activity[4].
In vitro, BRACO 19 trihydrochloride (0-40μM) treatment of eGFP-transfected HEK293 cells for 12h dose-dependently reduced the intracellular AdV viral growth[5]. Treatment of human uterine cancer cell line UXF1138L cells with BRACO 19 trihydrochloride (1μM) for 24h significantly reduced the expression of telomerase reverse transcriptase (hTERT) in the nucleus[6].
In vivo, oral treatment of UXF1138L cell xenograft mice with BRACO 19 trihydrochloride (5mg/kg) for 3 weeks did not significantly inhibit tumor growth, but significantly decreased the level of hTERT in tumor cells[6].
References:
[1] Gowan S M, Harrison J R, Patterson L, et al. A G-quadruplex-interactive potent small-molecule inhibitor of telomerase exhibiting in vitro and in vivo antitumor activity[J]. Molecular pharmacology, 2002, 61(5): 1154-1162.
[2] Jayaprasad A G, Chandrasekharan A, Jyothi S P A, et al. Telomerase inhibitors induce mitochondrial oxidation and DNA damage-dependent cell death rescued by Bcl-2/Bcl-xL[J]. International Journal of Biological Macromolecules, 2024, 264: 130151.
[3] Schmidt A, Liu M. Recent advances in the chemistry of acridines[J]. Advances in heterocyclic chemistry, 2015, 115: 287-353.
[4] Perrone R, Butovskaya E, Daelemans D, et al. Anti-HIV-1 activity of the G-quadruplex ligand BRACO-19[J]. Journal of antimicrobial chemotherapy, 2014, 69(12): 3248-3258.
[5] Majee P, Shankar U, Pasadi S, et al. Genome-wide analysis reveals a regulatory role for G-quadruplexes during Adenovirus multiplication[J]. Virus research, 2020, 283: 197960.
[6] Burger A M, Dai F, Schultes C M, et al. The G-quadruplex-interactive molecule BRACO-19 inhibits tumor growth, consistent with telomere targeting and interference with telomerase function[J]. Cancer research, 2005, 65(4): 1489-1496.
BRACO 19 trihydrochloride是一种有效的端粒酶/端粒抑制剂，IC50值为115±18nM，可防止端粒酶的加帽和催化作用[1]。BRACO 19 trihydrochloride是一种吖啶类化合物，可作为四联体（GQ）结合配体，稳定GQ四联体在3V端粒DNA处的形成，导致快速衰老或选择性细胞死亡[2]。BRACO 19 trihydrochloride是一种癌细胞增殖抑制剂[3]。BRACO 19 trihydrochloride具有抗HIV-1病毒活性[4]。
在体外，BRACO 19 trihydrochloride（0-40μM）处理eGFP转染的HEK293细胞12h，剂量依赖性地减少了细胞内AdV病毒的生长[5]。BRACO 19 trihydrochloride（1μM）处理人子宫癌细胞系UXF1138L细胞24h，显著降低了细胞核内端粒酶逆转录酶（hTERT）的表达[6]。
在体内，BRACO 19 trihydrochloride（5mg/kg）通过口服治疗UXF1138L细胞异种移植小鼠3周，对肿瘤生长抑制不显著，但肿瘤细胞中的hTERT水平显著下降[6]。
| Cell experiment [1]: | |
Cell lines | HEK293 cells |
Preparation Method | The HEK293 cells were infected with the virus at a multiplicity of infection (MOI) of 3 by the adsorption process at 37°C for 1h. The inoculum was then removed and was replaced by DMEM supplemented with 2% FBS and 1X PS. Subsequently, the infected cells were treated with 0-40μM BRACO 19 trihydrochloride and incubated at 37°C in a humidified CO2 chamber. Infection was measured as viral production, quantified by capturing fluorescent images at an interval of 12h using the Nikon Eclipse Ti-U inverted microscope system. |
Reaction Conditions | 0-40μM; 12h |
Applications | BRACO 19 trihydrochloride impairs AdV production in HEK293 cells. |
References: | |
| Cas No. | 1177798-88-7 | SDF | |
| Canonical SMILES | O=C(CCN5CCCC5)NC3=CC2=NC1=CC(NC(CCN6CCCC6)=O)=CC=C1C(NC4=CC=C(N(C)C)C=C4)=C2C=C3.Cl.Cl.Cl | ||
| 分子式 | C35H43N7O2.3HCl | 分子量 | 703.14 |
| 溶解度 | DMSO : 50 mg/mL (71.11 mM; ultrasonic and warming and heat to 80°C); H2O : 22 mg/mL (31.29 mM; Need ultrasonic and warming) | 储存条件 | Store at -20°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4222 mL | 7.111 mL | 14.2219 mL |
| 5 mM | 0.2844 mL | 1.4222 mL | 2.8444 mL |
| 10 mM | 0.1422 mL | 0.7111 mL | 1.4222 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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