567860
SRT1720
SRT1720, CAS 925434-55-5, is a cell-permeable inhibitor of the mitochondrial SIRT3. Inhibition is AceCS2-competitive (Ki = 0.56 µM; Km = 2.44 µM), but NAD+-uncompetitive (Ki = 0.34 µM; Km = 280 µM).
别名:
SRT1720, HAT抑制剂XI，组蛋白乙酰转移酶抑制剂XI，p300/CBP抑制剂IX，N-(2-(3-(1-(哌嗪基甲基)咪唑并[2,1-b]噻唑-6-基)苯基] -2-喹啉甲酰胺，Sirtuin -3抑制剂，SRT1720，SIRT3抑制剂II
质量水平
方案
≥97% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 2.5 mg/mL, clear, yellow
运输
ambient
储存温度
−20°C
SMILES字符串
O=C(C1=NC(C=CC=C2)=C2N=C1)NC3=CC=CC=C3C4=CN5C(SC=C5CN6CCNCC6)=N4
InChI
1S/C25H23N7OS/c33-24(22-13-27-20-7-3-4-8-21(20)28-22)29-19-6-2-1-5-18(19)23-15-32-17(16-34-25(32)30-23)14-31-11-9-26-10-12-31/h1-8,13,15-16,26H,9-12,14H2,(H,29,33)
InChI key
IASPBORHOMBZMY-UHFFFAOYSA-N
一般描述
一种细胞渗透性喹啉甲酰胺化合物，可以底物AceCS2竞争性的方式抑制（Ki = 0.56 µM；Km = 2.44 µM）线粒体SIRT3，但对NAD+是以非竞争性（Ki = 0.34 µM；Km = 280 µM）的方式进行抑制的。还据报道可在体外降低细胞p53 Lys382乙酰化（在U2OS和MEF培养中有效浓度= 10 µM）并抑制p300 HAT活性（IC50 = 9 µM），以及在体内对几种鼠类和啮齿类2型糖尿病模型提供治疗作用。SRT1720是否以及如何激活SIRT1活性仍不确定。也可以提供25 mM的DMSO溶液（目录号530748）。
包装
用惰性气体包装
其他说明
Baur, J.A., et al. 2012.Nat. Rev. Drug Discov.11, 443.
Minor, R.K., et al. 2011.Sci. Rep.1, 70.
Huber, J.L., et al. 2010.Future Med. Chem.2, 1751
Pacholec, M., et al. 2010.J. Biol. Chem.285, 8340
Jin, L., et al. 2009.Protein Sci.18, 514
Feige, J.N., et al. 2008.Cell Metab.8, 347
Milne, J.C., et al. 2007.Nature450, 712.
Minor, R.K., et al. 2011.Sci. Rep.1, 70.
Huber, J.L., et al. 2010.Future Med. Chem.2, 1751
Pacholec, M., et al. 2010.J. Biol. Chem.285, 8340
Jin, L., et al. 2009.Protein Sci.18, 514
Feige, J.N., et al. 2008.Cell Metab.8, 347
Milne, J.C., et al. 2007.Nature450, 712.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：监管审查（Z）
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Audrey Laurent et al.
Life science alliance, 5(7) (2022-03-31)
Methylation and demethylation of cytosines in DNA are believed to act as keystones of cell-specific gene expression by controlling the chromatin structure and accessibility to transcription factors. Cancer cells have their own transcriptional programs, and we sought to alter such
Seon Beom Song et al.
Cells, 10(3) (2021-04-04)
Mitochondrial autophagy (or mitophagy) is essential for mitochondrial quality control, which is critical for cellular and organismal health by attenuating reactive oxygen species generation and maintaining bioenergy homeostasis. Previously, we showed that mitophagy is activated in human cells through SIRT1
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