JGB1741

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JGB1741

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1256375-38-8

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
25mg	电议

产品介绍

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 是一种弱 SIRT2 和 SIRT3 抑制剂，IC50>100 μM。 JGB1741 通过调节 Bax/Bcl2 比率、细胞色素 c 释放和 PARP 裂解增加乙酰化 p53 水平，从而导致 p53 介导的细胞凋亡。 JGB1741具有乳腺癌研究的潜力。

Cas No.	1256375-38-8
别名	ILS-JGB-1741
化学名	4,5,6,7-tetrahydro-2-[(E)-[(2-hydroxy-1-naphthalenyl)methylene]amino]-N-(phenylmethyl)-benzo[b]thiophene-3-carboxamide
Canonical SMILES	OC1=C(/C=N/C2=C(C(NCC3=CC=CC=C3)=O)C(CCCC4)=C4S2)C(C=CC=C5)=C5C=C1
分子式	C₂₇H₂₄N₂O₂S
分子量	440.6
溶解度	≤0.2mg/ml in DMSO;0.14mg/ml in dimethyl formamide
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.