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).

• 別名: SRT1720, HAT Inhibitor XI, Histone Acetyltransferase Inhibitor XI, p300/CBP Inhibitor IX, N-(2-(3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-quinolinecarboxamide, Sirtuin-3 Inhibitor, SRT1720, SIRT3 Inhibitor II, HAT Inhibitor XI, Histone Acetyltransferase Inhibitor XI, p300/CBP Inhibitor IX, SIRT3 Inhibitor II, N-(2-(3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-quinolinecarboxamide, Sirtuin-3 Inhibitor, SRT1720
• 実験式（ヒル表記法）: C₂₅H₂₃N₇OS
• CAS番号: 925434-55-5
• 分子量: 469.56
• MDL番号: MFCD14584468
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 2.5 mg/mL, clear, yellow
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: 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

詳細

詳細

A cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2- (Acetyl-CoA synthetase 2) competitive (K_i = 0.56 µM; K_m = 2.44 µM; V_max = 173.35 µM/min), but NAD⁺-uncompetitive (K_i = 0.34 µM; K_m = 280 µM; V_max = 0.86 µM/min), manner, indicative of NAD⁺ binding as a prerequisite for inhibitor binding. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 µM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC₅₀ = 9 µM) in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.) in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain.

A cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2-competitive (K_i = 0.56 µM; K_m = 2.44 µM), but NAD⁺-uncompetitive (K_i = 0.34 µM; K_m = 280 µM), manner. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 µM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC₅₀ = 9 µM) in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.) in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain. Also available as a 25 mM solution in DMSO (Cat. No. 530748).

包装

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable