JGB1741(Synonyms: ILS-JGB-1741)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JGB1741 (Synonyms: ILS-JGB-1741)

JGB1741 (ILS-JGB-1741) 是一种有效且特异性的 SIRT1 活性抑制剂，IC50 为 ~15 μM。JGB1741 对 SIRT2 和 SIRT3 具有弱的抑制作用，IC50>100 μM。JGB1741 通过调节 Bax/Bcl2 比率、细胞色素 c 释放和 PARP 裂解来增加乙酰化 p53 水平，导致 p53 介导的细胞凋亡。JGB1741 具有用于乳腺癌研究的潜力。

JGB1741(Synonyms: ILS-JGB-1741)

JGB1741 Chemical Structure

CAS No. : 1256375-38-8

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生物活性

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>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 research[1].

IC50 & Target[1]

SIRT1

∼15 μM (IC50)

SIRT2

>100 μM (IC50)

SIRT3

>100 μM (IC50)

体外研究
(In Vitro)

JGB1741 (ILS-JGB-1741; 1-10000 nM; 24 h) inhibits MDA-MB 231 cell proliferation[1].
JGB1741 (0.01-1 μM; 24 h) induces apoptosis of MDA-MB 231 cells[1].
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[1].
JGB1741 (0.01-1 μM; 24 h) shows an increase in the global acetylation of H3K9, p53 expression and acetylated p53K382 levels[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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[1]

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[1]

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.

分子量

440.56

Formula

C27H24N2O2S
CAS 号

1256375-38-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Arunasree M Kalle, et al. Inhibition of SIRT1 by a small molecule induces apoptosis in breast cancer cells. Biochem Biophys Res Commun. 2010 Oct 8;401(1):13-9.

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