基本信息

技术规格

物性(参考值)

产品说明

一般描述

A cell-permeable and selective inhibitor of NAD⁺-dependent deacetylase activity of Sir2 protein (IC₅₀ = 60 µM). Creates a phenocopy of the sir2 deletion mutant in S. cerevisiae and sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Reported to act by either altering or blocking access to the acetylated histone-binding pocket.
A cell-permeable lactone derived from β-naphthol that acts as a selective inhibitor of NAD⁺-dependent histone deacetylase activity of Sir2 protein (IC₅₀ = 60 µM). It creates a conditional phenocopy of a sir2 deletion mutant in S. cerevisiae and sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Acts by either altering or blocking access to the acetylated histone binding pocket.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
NAD⁺-dependent histone deacetylase activity of Sir2 protein
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 60 µM against NAD+-dependent histone deacetylase activity of Sir2 protein

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Bedalov, A., et al. 2001. Proc. Natl. Acad. Sci. USA98, 15113.

法律信息

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

基本信息

产品性质

安全信息

产品说明

应用

Splitomicin was used to inhibit SIRT1 in human aortic endothelial cells and sirtuins in human breast cancer cells. Mouse leukaemic monocyte macrophage cell line was treated with Splitomicin prior to cholesterol efflux studies.

包装

5 mg in glass bottle

生化/生理作用

Splitomicin, a derivative of β-naphthol is an inhibitor of Silent Information Regulator 2 (SIR2). It inhibits the NAD⁺-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase, interferes with mobilization of intracellular Ca⁺² and ATP release. This results in inhibition of platelet aggregation that is effective in cardiovascular and cerebrovascular diseases.
Sir2p (silent information regulator) and HDAC inhibitor.

特点和优势

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基本信息

产品性质

安全信息

基本信息