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.
Cas No.: 14513-15-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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.
Average Rating: 5
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