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
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关于此项目
经验公式（希尔记法）:
C25H23N7OS
化学文摘社编号:
分子量:
469.56
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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)
SMILES string
O=C(C1=NC(C=CC=C2)=C2N=C1)NC3=CC=CC=C3C4=CN5C(SC=C5CN6CCNCC6)=N4
InChI key
IASPBORHOMBZMY-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 2.5 mg/mL, clear, yellow
shipped in
ambient
storage temp.
−20°C
Quality Level
相关类别
General description
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）。
Packaging
用惰性气体包装
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：监管审查（Z）
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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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