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).

• Szinonimák: 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
• Tapasztalati képlet (Hill-képlet): C₂₅H₂₃N₇OS
• CAS-szám: 925434-55-5
• Molekulatömeg: 469.56
• MDL-szám: MFCD14584468
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥97% (HPLC)
• form: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: yellow
• oldhatóság: DMSO: 2.5 mg/mL, clear, yellow
• kiszállítva: ambient
• tárolási hőmérséklet: −20°C
• SMILES string: 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)
• Nemzetközi kémiai azonosító kulcs: IASPBORHOMBZMY-UHFFFAOYSA-N

Leírás

Általános leírás

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).

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Regulatory Review (Z)

Egyéb megjegyzések

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.

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable