Home >> SIRT1/2 Inhibitor IV
Related Products
SIRT1/2 Inhibitor IV SIRT1 and SIRT2 inhibitor

Catalog No.B6063
Size Price Stock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$95.00
In stock
10mg
$175.00
In stock
25mg
$375.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

SIRT1/2 Inhibitor IV

SIRT1/2 Inhibitor IV Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

SIRT1/2 Inhibitor IV Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 14513-15-6 SDF Download SDF
Chemical Name 5-((2-hydroxynaphthalen-1-yl)methyl)-2-mercapto-6-phenylpyrimidin-4-ol
Canonical SMILES OC(C=CC1=CC=CC=C12)=C2CC(C(O)=NC(S)=N3)=C3C4=CC=CC=C4
Formula C21H16N2O2S M.Wt 360.43
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

SIRT1/2 Inhibitor IV (cambinol) is a small-molecule inhibitor of SIRT1 and SIRT2 with IC50 values of 56 ?M and 59 ?M, respectively [1].

Sirtuin 1 (SIRT1) and SIRT2 are NAD-dependent deacetylases and are members of sirtuin family protein. SIRT1 regulate pathways in metabolism, inflammation and tumorigenesis and SIRT2 functions as a tubulin deacetylase[2].

SIRT1/2 Inhibitor IV is a cell-permeable SIRT1 and SIRT2 inhibitor. SIRT1/2 Inhibitor IV inhibited human SIRT1 and SIRT2 NAD-dependent deacetylase activity with IC50 values of 56 and 59 ?mol/L, respectively. In NCI H460 lung cancer cell line, combined inhibition of SIRT2 and HDAC6 with SIRT1/2 Inhibitor IV and trichostatin A resulted in hyperacetylation of tubulin. SIRT1/2 Inhibitor IV also increased acetylation of p53. In p53-positive lung cancer cell line NCI H460, SIRT1/2 Inhibitor IV mediated inhibition of SIRT1 sensitized cells to etoposide in p53-independent manner [1].

In a mouse xenograft model, SIRT1/2 Inhibitor IV (100 mg/kg) administered i.v. into the tail vein or i.p. daily for 2 weeks (five injections per week) reduced tumor growth [1]. In mice pre-treated with cambinol for 2 hours and then exposed to 6% oxygen for 6 hours, cambinol significantly reduced EPO mRNA in the kidney and the liver [2].

References:
Heltweg B, Gatbonton T, Schuler AD, et al.  Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. Cancer Res. 2006 Apr 15;66(8):4368-77.
Laemmle A, Lechleiter A, Roh V, et al.  Inhibition of SIRT1 impairs the accumulation and transcriptional activity of HIF-1α protein under hypoxic conditions. PLoS One. 2012;7(3):e33433.