SIRT1/2 Inhibitor IV (Synonyms: Cambinol,NSC 112546,SIRT1 Inhibitor II,SIRT2 Inhibitor VI) |
| رقم الكتالوجGC11716 |
مثبط SIRT1 / 2 IV هو مثبط SIRT1 و SIRT2 بقيم IC50 56 μ ؛ M و 59 μ ؛ M ، على التوالي. مثبط SIRT1 / 2 IV هو مثبط قوي لسفينجوميليناز (N-SMase) مخترق قوي للدماغ (مثبط خارجي).
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.
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SIRT1/2 Inhibitor IV is a cell-permeable inhibitor of SIRT1 and SIRT2 with IC50 values of 56 μM and 59 μM, respectively [1].
Sirtuin proteins are nicotinamide adenine dinucleotide (NAD+)-dependent deacetylases. They play important roles in control of cellular responses to stress and in tumorigenesis through deacetylation of important regulatory proteins, including p53 and the BCL6 oncoprotein. SIRT1 and SIRT2 exist in both the nucleus and cytoplasm. SIRT1 regulate pathways in metabolism, inflammation and tumorigenesis and SIRT2 functions as a tubulin deacetylase [1][2].
SIRT1/2 Inhibitor IV (Cambinol) is a cell-permeable sirtuin inhibitor that inhibits human SIRT1 and SIRT2 NAD+-dependent deacetylase activity with IC50 values of 56 μM and 59 μM, respectively, and has only weak inhibitory activity against SIRT5 (42% inhibition at 300 μmol/L). In NCI H460 lung cancer cell line, Cambinol inhibited SIRT1 and SIRT2 deacetylase activity, and also increased p53 activation during DNA damage response [1]. In HepG2 cells, Cambinol inhibited SIRT activity, which led to a dose-dependent repression of HIF-1a protein accumulation [2].
In nonobese diabetic/severe combined immunodeficient mice xenografted Daudi cells, cambinol at the dose of 100 mg/kg reduced tumor growth without inducing obvious toxicity [1].
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.
Cell experiment: | .The reporter construct with or without varying amounts of GAL4-BCL6 expression plasmid are introduced into NCI-H460 cells using calcium phosphate method. A plasmid containing cytomegalovirus (CMV)-driven β-galactosidase reporter (50 ng) is cotransfected to control for transfection efficiency. Sixteen hours after transfection, cells are treated with 100 μM cambinol of DMSO (control) for 24 hours and the luciferase and β-galactosidase activity is measured[1]. |
Animal experiment: | Mice: Cambinolat the dose of 100 mg/kg, or vehicle are administered i.v. through tail vein injection or i.p. daily from day 5 to 19 (five injections per week). The dose of 100 mg/kg cambinol is the highest dose that could be administered as a single i.v. injection due to limited solubility of the drug. Tumor size is measured thrice a week using caliper and the tumor volumes are calculated[1]. |
References: [1]. Heltweg B, 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. | |
| Cas No. | 14513-15-6 | SDF | |
| المرادفات | Cambinol,NSC 112546,SIRT1 Inhibitor II,SIRT2 Inhibitor VI | ||
| Chemical Name | 2,3-dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone | ||
| Canonical SMILES | S=C1NC(C(CC2=C(C=CC=C3)C3=CC=C2O)=C(C4=CC=CC=C4)N1)=O | ||
| Formula | C21H16N2O2S | M.Wt | 360.4 |
| الذوبان | 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 | -20°C, protect from light |
| 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7747 mL | 13.8735 mL | 27.7469 mL |
| 5 mM | 554.9 μL | 2.7747 mL | 5.5494 mL |
| 10 mM | 277.5 μL | 1.3873 mL | 2.7747 mL |
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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.
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- Purity: >99.00%
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