SPLITOMICIN Chemical Properties

Melting point:

73-74.5℃

storage temp. 

2-8°C

solubility 

insoluble in H2O; ≥44.2 mg/mL in EtOH with ultrasonic; ≥9.05 mg/mL in DMSO

form 

solid

color 

White to Almost white

Safety Information

WGK Germany 

3

HS Code 

2932.20.4500

MSDS

• Language:English Provider:SigmaAldrich

SPLITOMICIN Usage And Synthesis

Uses

Splitomicin is a selective and potent inhibitor of Sir2 (silent information regulator 2), producing an inhibitory effect on neutrophils. Acts as an anti-inflammatory agent.

Definition

ChEBI: A benzochromenone that is 2,3-dihydro-1H-benzo[f]chromene substituted by an oxo group at position 3. It has been found to exhibit potential inhibitory activity against Sir2 proteins.

Synthesis Reference(s)

Journal of the American Chemical Society, 69, p. 2341, 1947 DOI: 10.1021/ja01202a027

General Description

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.

Biological Activity

Inhibitor of Sir2p (IC 50 = 60 μ M), an NAD + -dependent Sir2 family deacetylase required for chromatin-dependent silencing in yeast.

Biochem/physiol Actions

Cell permeable: yes

storage

+4°C

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