567750
Splitomicin
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).
Synonyme(s) :
Splitomicin, 1,2-Dihydro-3H-naphtho[2,1-b]pyran-3-one
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A propos de cet article
Formule empirique (notation de Hill) :
C13H10O2
Numéro CAS:
Poids moléculaire :
198.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Service technique
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assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
O1c2c(c3c(cc2)cccc3)CCC1=O
InChI
1S/C13H10O2/c14-13-8-6-11-10-4-2-1-3-9(10)5-7-12(11)15-13/h1-5,7H,6,8H2
InChI key
ISFPDBUKMJDAJH-UHFFFAOYSA-N
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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
NAD+-dependent histone deacetylase activity of Sir2 protein
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
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Bedalov, A., et al. 2001. Proc. Natl. Acad. Sci. USA98, 15113.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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