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567860

SRT1720

Name: SRT1720
Brand: MM

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

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この商品について

実験式（ヒル表記法）:

C₂₅H₂₃N₇OS

CAS番号:

925434-55-5

分子量:

469.56

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD14584468

Assay:

≥97% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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特性

Quality Segment

100

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

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)

InChI key

IASPBORHOMBZMY-UHFFFAOYSA-N

詳細

General description

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).

Packaging

Packaged under inert gas

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.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

保管分類

11 - Combustible Solids

一体何が起きているの？

WGK 3

引火点 (F)

Not applicable

引火点（°C）