JGB1741

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JGB1741 是一种有效的选择性 SIRT1 抑制剂，IC50 为 15 μM。 JGB1741 调节 Bax/Bcl2 比率、细胞色素 c 释放和 PARP 裂解，并增加乙酰化 p53 水平，导致 p53 介导的细胞凋亡。 JGB1741可用于乳腺癌研究。

JGB1741 is a potent and selective inhibitor of SIRT1 with an IC50 of 15 μM. JGB1741 modulates Bax/Bcl2 ratio, cytochrome c release and PARP cleavage and increases the acetylated p53 levels leading to p53-mediated apoptosis. JGB1741 can be used in studies about breast cancer.(In Vitro):JGB1741 (1-10000 nM) inhibits the cell proliferation of K562, HepG2 and MDA-MB 231 cell lines. JGB1741 (0.01-1 μM) induces apoptosis of MDA-MB 231 and shows a cell cycle arrest at G1 phase with more cells entering into sub G0/G1 phase. JGB1741 (0.01-1 μM) increases the global acetylation of H3K9, acetylated p53K382 levels and p53 expression.

JGB1741 (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. Cell Proliferation Assay Cell 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 IC50 of 0.5 μM than K562 and HepG2 cell proliferation (IC50>1 μM).Apoptosis Analysis Cell 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 Analysis Cell 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 Analysis Cell 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.

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ILS-JGB-1741

Chromatin/Epigenetic

Sirtuin

Aurora B

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1256375-38-8

440.56

C27H24N2O2S

>98% (HPLC)

In Vitro:?DMSO : 5 mg/mL (11.35 mM)

C(NCC1=CC=CC=C1)(=O)C=2C3=C(SC2/N=C/C=4C5=C(C=CC4O)C=CC=C5)CCCC3

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(-20℃)

With Ice Pack

≥ 2 years