Splitomicin (CAS 5690-03-9)

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Synonym:	1,2-Dihydro-3H-naphtho[2,1-b]pyran-3-one; 1-Naphthalen propanoic acid
Application:	A Sir2 inhibitor
CAS Number:	5690-03-9
Purity:	≥98%
Molecular Weight:	198.2
Molecular Formula:	C₁₃H₁₀O₂

Description

Splitomicin is a cell-permeable lactone that acts as a selective inhibitor of Sir2 by targeting its NAD⁺ dependent histone deacetylase activity. Splitomicin 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. Splitomicin acts by either altering or blocking access to the acetylated histone binding pocket.

Technical Information

Appearance:	Off-white powder
Physical State:	Solid
Solubility:	Soluble in DMSO (100 mM), and ethanol (100 mM).
Storage:	Store at 4° C
Melting Point:	50-52 °C
Boiling Point:	383.57 °C at 760 mmHg (Predicted)
Density:	1.26 g/cm³ (Predicted)
Refractive Index:	n²⁰_D 1.66 (Predicted)
IC50:	NAD+-dependent histone deacetylase activity of Sir2 protein: IC₅₀ = 60 µM; Histone deacetylase: IC₅₀ = >10000 nM (Plasmodium falciparum); NAD-dependent histone deacetylase SIR2: IC₅₀ = 74000 nM (Saccharomyces cerevisiae S288c)

Safety and Reference Information

WGK Germany:	3
PubChem CID:	5269
MDL Number:	MFCD08705254
SMILES:	C1CC(=O)OC2=C1C3=CC=CC=C3C=C2

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

References

1. Bedalov, A., et al. 2001. Proc. Natl. Acad. Sci. USA 98: 15113-15118. PMID: 11752457

SDS

Datasheet/SDS