JGB1741 (Synonyms: ILS-JGB-1741) |
| Catalog No.GC13062 |
JGB1741 (ILS-JGB-1741) es un inhibidor potente y especÍfico de la actividad de SIRT1 con una IC50 de ~15 μM. JGB1741 es un inhibidor débil de SIRT2 y SIRT3 con una IC50 >100 μM. JGB1741 aumenta los niveles de p53 acetilados que conducen a la apoptosis mediada por p53 con modulaciÓn de la relaciÓn Bax/Bcl2, liberaciÓn de citocromo c y escisiÓn de PARP. JGB1741 tiene potencial para la investigaciÓn del cÁncer de mama.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1256375-38-8
Sample solution is provided at 25 µL, 10mM.
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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.
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