Sirtinol

ALX-270-308

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SIRT inhibitor

Specific cell permeable inhibitor of the sirtuin family of NAD-dependent deacetylases (ySir2: IC₅₀=48µM; hSIRT1: IC₅₀=60µM; hSIRT2: IC₅₀=58µM) with no effect on human HDAC1. Reported to inhibit Sir2p transcriptional silencing activity in vivo (IC₅₀=25µM) and NAD-dependent histone deacetylase activity of purified recombinant yeast Sir2p (IC₅₀=70µM) and hSIRT2 (IC₅₀=40µM) in vitro.

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Product Details

Alternative Name	Sir Two Inhibitor Naphthol, 2-[(2-Hydroxynaphthalen-1-yl-methylene)amino]-N-(1-phenethyl)benzamide
Appearance	Off-white to yellow crystals.
CAS	410536-97-9
Couple Target	SIRT
Couple Type	Inhibitor
Formula	C₂₆H₂₂N₂O₂
Identity	NMR
MW	394.5
Purity	≥97% (HPLC)
Solubility	Soluble in DMSO, 100% ethanol or dimethyl formamide.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Relatively unstable in aqueous solution, especially at acidic pH.
Handling	Protect from moisture. Protect from light. Store under inert gas.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

High glucose-induced oxidative stress represses sirtuin deacetylase expression and increases histone acetylation leading to neural tube defects: Yu, J., Wu, Y., et al.; J. Neurochem. 137, 371 (2016), Abstract
Reduced expression of epidermal growth factor receptor, E-cadherin, and occludin in the skin of flaky tail mice is due to filaggrin and loricrin deficiencies: K. Nakai, et al.; Am. J. Pathol. 181, 969 (2012), Abstract
Inhibition of SIRT1 impairs the accumulation and transcriptional activity of HIF-1α protein under hypoxic conditions: Laemmle, A., Lechleiter, A., et al.; PLoS One 7, e33433 (2012), Abstract
SIRT1 regulation of apoptosis of human chondrocytes: K. Takayama, et al.; Arthritis Rheum. 60, 2731 (2009), Abstract — Full Text
Identification and characterization of novel sirtuin inhibitor scaffolds: B.D. Sanders, et al.; Bioorg. Med. Chem. 17, 7031 (2009), Abstract
Sirt1 inhibitor, Sirtinol, induces senescence-like growth arrest with attenuated Ras-MAPK signaling in human cancer cells: H. Ota, et al.; Oncogene 25, 176 (2006), Abstract
Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors: A. Mai, et al.; J. Med. Chem. 48, 7789 (2005), Abstract
Nonisotopic substrate for assaying both human zinc and NAD+-dependent histone deacetylases: B. Heltweg, et al.; Anal. Biochem. 319, 42 (2003), Abstract
Human telomeric position effect is determined by chromosomal context and telomeric chromatin integrity: C.E. Koering, et al.; EMBO Rep. 3, 1055 (2002), Abstract — Full Text
Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening: C.M. Grozinger, et al.; J. Biol. Chem. 276, 38837 (2001), Abstract — Full Text

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Sirtinol

ALX-270-308

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Handling & Storage

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