JGB1741 (C09-1140-937)

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC 50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC 50 >100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer researchIn VitroJGB1741 (ILS-JGB-1741; 1-10000 nM; 24 h) inhibits MDA-MB 231 cell proliferation. JGB1741 (0.01-1 μM; 24 h) induces apoptosis of MDA-MB 231 cells. JGB1741 (0.01-1 μM; 24 h) shows a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase. JGB1741 (0.01-1 μM; 24 h) shows an increase in the global acetylation of H3K9, p53 expression and acetylated p53K382 levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: K562, HepG2 and MDA-MB 231 cell lines Concentration: 1, 10, 50, 100, 500, 1000, 10000 nM Incubation Time: 24 hours Result: Inhibited MDA-MB 231 cell proliferation more potently with an IC 50 of 0.5 μM than K562 and HepG2 cell proliferation (IC 50 >1 μM). Apoptosis AnalysisCell Line: MDA-MB 231 cells Concentration: 0.01, 0.1, 0.5, 1 μM Incubation Time: Result: Showed an increase in the percent apoptotic cells in a dose-dependent fashion with ∼70% apoptosis at 1 μM concentration. Cell Cycle AnalysisCell Line: MDA-MB 231 cells Concentration: 0.01, 0.1, 0.5, 1 μM Incubation Time: Result: Showed a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase, the apoptotic phase, in a dose-dependent fashion. Western Blot AnalysisCell Line: MDA-MB 231 cells Concentration: 0.01, 0.1, 0.5, 1 μM Incubation Time: Result: Caused a dose-dependent increase in the global acetylation of H3K9. Showed an increase in both p53 expression and acetylated p53K382 levels.Form:SolidIC50& Target:SIRT1 ∼15 μM (IC 50 ) SIRT2 >100 μM (IC 50 ) SIRT3 >100 μM (IC 50 ). Specification: 0.99 Molecular Formula: C27H24N2O2S Molecular Weight: 440.56