Splitomicin

Names

[ Name ]:
Splitomicin

[Synonym ]:
Splitomicin
1,2-dihydrobenzo[f]chromen-3-one
1,2-Dihydro-3H-benzo[f]chromen-3-one
MFCD03792600
3H-Naphtho[2,1-b]pyran-3-one, 1,2-dihydro-

Biological Activity

[Description]:

Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

[Target]

Sir2p:60 μM (IC50)

[In Vivo]

Splitomicin (80 mg/kg with an intraperitoneal injection every 24 h for 5 days, in mice) enhances tissue factor (TF) activity in the arterial vessel wall and accelerates carotid artery thrombus formation in a photochemical injury model[2]. Animal Model: C57BL/6 mice aged 12-14 weeks weighing on average 27 g[2] Dosage: 80 mg/kg Administration: Intraperitoneal injection every 24 h for 5 days Result: Increased TF activity in mouse carotid artery as compared with the controls.

[References]

[1]. Bedalov A, et al. Identification of a small molecule inhibitor of Sir2p. Proc Natl Acad Sci U S A. 2001 Dec 18;98(26):15113-8.

[2]. Breitenstein A, et al. Sirt1 inhibition promotes in vivo arterial thrombosis and tissue factor expression in stimulated cells. Cardiovasc Res. 2011 Feb 1;89(2):464-72.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
383.6±17.0 °C at 760 mmHg

[ Melting Point ]:
73-74.5℃

[ Molecular Formula ]:
C₁₃H₁₀O₂

[ Molecular Weight ]:
198.217

[ Flash Point ]:
161.2±18.4 °C

[ Exact Mass ]:
198.068085

[ PSA ]:
26.30000

[ LogP ]:
3.03

[ Appearance of Characters ]:
solid

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.656

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2914399090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2914399090

[ Summary ]:
2914399090. other aromatic ketones without other oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:5.5%. General tariff:30.0%

Articles

SIRT1 decreases Lox-1-mediated foam cell formation in atherogenesis.

Eur. Heart J. 31 , 2301-9, (2010)

Endothelial activation, macrophage infiltration, and foam cell formation are pivotal steps in atherogenesis. Our aim in this study was to analyse the role of SIRT1, a class III deacetylase with import...

Synergistic activation of HIV-1 expression by deacetylase inhibitors and prostratin: implications for treatment of latent infection.

PLoS ONE 4(6) , e6093, (2009)

The persistence of transcriptionally silent but replication-competent HIV-1 reservoirs in Highly Active Anti-Retroviral Therapy (HAART)-treated infected individuals, represents a major hurdle to virus...

Sirt1 inhibition promotes in vivo arterial thrombosis and tissue factor expression in stimulated cells.

Cardiovasc. Res. 89 , 464-72, (2011)

The mammalian silent information regulator-two 1 (Sirt1) blunts the noxious effects of cardiovascular risk factors such as type 2 diabetes mellitus and obesity. Nevertheless, the role of Sirt1 in regu...