JGB1741

A SIRT1 inhibitor

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库存: 现货

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1mg

￥750.00

600.00

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5mg

￥3362.00

2690.00

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10mg

￥5337.00

4270.00

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25mg

￥10550.00

8440.00

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货号: ajci10366
CAS: 1256375-38-8
别名: ILS-JGB-1741
分子式: C27H24N2O2S
分子量: 440.6
纯度: >98%
溶解度: ≤0.2mg/ml in DMSO;0.14mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.