JGB1741
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mg | ¥975.00 | 10-15工作日发货 | |
| 5mg | ¥3697.00 | 10-15工作日发货 | |
| 10mg | ¥5917.00 | 10-15工作日发货 | |
| 25mg | ¥12426.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
JGB1741 is a small molecule SIRT1 inhibitor [1].
Sirtuins or Sir2 (silent information regulator 2)-related enzymes have originally been defined as a family of nicotinamide adenine dinucleotide-dependent enzymes which are involved in deacetylating lysine residue on multiple proteins. The sirtuins show highly conservation from archaebacteria to eukaryotes. The mammalian sirtuins SIRT1–SIRT7 have been implicated in a variety of cellular functions, such as gene silencing, over the control of the cell cycle and apoptosis, to energy homeostasis [2].
In vitro: JGB1741 potently inhibited the proliferation of human metastatic breast cancer cells, MDA-MB 231. JGB1741 showed antitumor effects on three different cancer cell lines, K562, HepG2 and MDA-MB 231 with an IC50 of 1, 10 and 0.5 μM, respectively. JGB1741-induced apoptosis has been associated with increase in cytochrome c release, modulation in Bax/Bcl2 ratio and cleavage of PARP [1].
References:
[1] Kalle A M, Mallika A, Badiger J, et al. Inhibition of SIRT1 by a small molecule induces apoptosis in breast cancer cells[J]. Biochemical and biophysical research communications, 2010, 401(1): 13-19.
[2] Yamamoto H, Schoonjans K, Auwerx J. Sirtuin functions in health and disease[J]. Molecular Endocrinology, 2007, 21(8): 1745-1755.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 1256375-38-8 |
| 分子式 | C27H24N2O2S |
| 分子量 | 440.6 |
| 化学名称 | 4,5,6,7-tetrahydro-2-[(E)-[(2-hydroxy-1-naphthalenyl)methylene]amino]-N-(phenylmethyl)-benzo[b]thiophene-3-carboxamide |
| 溶解度 | ≤0.2mg/ml in DMSO;0.14mg/ml in dimethyl formamide |
| SMILES | Oc1c(/C=N/c2c(C(NCc3ccccc3)=O)c(CCCC3)c3[s]2)c(cccc2)c2cc1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | JGB1741(ILS-JGB-1741)是一种强效的特异性 SIRT1 活性抑制剂,其 IC50 为 ~15μM。JGB1741 是一种弱 SIRT2 和 SIRT3 抑制剂,其 IC50 均大于 100 μM。JGB1741 可提高乙酰化 p53 的水平,导致 p53 介导的细胞凋亡,并调节 Bax/Bcl2 比率、细胞色素 c 释放和 PARP 分裂。JGB1741 具有乳腺癌研究的潜力。 |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 1 篇科研文献
- 1. Udomruk S, Kaewmool C, et al. "Sesamin Promotes Neurite Outgrowth under Insufficient Nerve Growth Factor Condition in PC12 Cells through ERK1/2 Pathway and SIRT1 Modulation." Evid Based Complement Alternat Med. 2020;2020:9145458. PMID:32308720



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