Home>>Signaling Pathways>> Chromatin/Epigenetics>> Sirtuin>>SIRT1/2 Inhibitor IV

SIRT1/2 Inhibitor IV

Catalog No.GC17145

SIRT1 and SIRT2 inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

SIRT1/2 Inhibitor IV Chemical Structure

Cas No.: 14513-15-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$75.00
In stock
5mg
$68.00
In stock
10mg
$128.00
In stock
25mg
$284.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

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:
[1].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.
[2].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.

Chemical Properties

Cas No. 14513-15-6 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 DMF: 16 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml,Ethanol: 0.33 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7745 mL 13.8723 mL 27.7446 mL
5 mM 0.5549 mL 2.7745 mL 5.5489 mL
10 mM 0.2774 mL 1.3872 mL 2.7745 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for SIRT1/2 Inhibitor IV

Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for SIRT1/2 Inhibitor IV

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.