| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
SIRT7:325 nM (IC50)
SIRT7 inhibitor 97491 targets SIRT7 (sirtuin 7), a NAD+-dependent deacetylase that localizes to the nucleolus and regulates ribosomal RNA transcription, DNA repair, and cellular stress responses. SIRT7 has been implicated in cancer progression and tumorigenesis. By inhibiting SIRT7 with an IC50 of 325 nM, the compound increases p53 stability through acetylation at K373/382, thereby preventing tumor progression. SIRT7 inhibitor 97491 also promotes apoptosis through the caspase pathway. |
|---|---|
| ln Vitro |
The SIRT7 inhibitor 97491 (1–10 μM) inhibits MES-SA cell growth without harming HEK293 cells [1].
In vitro, SIRT7 inhibitor 97491 reduces the deacetylase activity of SIRT7 with an IC50 of 325 nM in a dose-dependent manner. It increases p53 stability through acetylation at K373/382 and promotes apoptosis through the caspase pathway. The compound inhibits MES-SA cell growth without harming HEK293 cells, suggesting some selectivity for cancer cells over normal cells. It has antitumor activity in various cancer models. |
| ln Vivo |
Tumor growth in xenograft mice is inhibited by SIRT7 inhibitor 97491 (2 mg/kg; intraperitoneally; for 3 weeks, excluding weekends) [1].
In vivo, SIRT7 inhibitor 97491 has antitumor activity. It induces expression of p53 and its acetylation by inhibiting SIRT7, and upregulates apoptotic effects through caspase-related proteins, inhibiting cancer growth. The compound prevents tumor progression by increasing p53 stability. However, specific in vivo efficacy data and dosing details have not been extensively detailed in the available literature. Further preclinical studies would be required. |
| Enzyme Assay |
For in vitro enzyme assays, recombinant SIRT7 protein is incubated with a peptide substrate (such as acetylated p53 peptide) and NAD+ in assay buffer. The test compound is added at various concentrations (0.1-1000 nM). Deacetylase activity is measured by monitoring the release of deacetylated product using fluorescence-based or mass spectrometry-based methods. IC50 values are calculated by fitting dose-response curves.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Human uterine sarcoma MES-SA cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Led to more than 50% decrease in cell proliferation at concentrations of 5 and 10 μM. Cell Cytotoxicity Assay[1] Cell Types: Human embryonic kidney cell line HEK293 cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: HEK293 cells were almost unaffected. For cell-based assays, cancer cell lines (such as MES-SA cells) are treated with SIRT7 inhibitor 97491 at concentrations ranging from 0.1-10 µM. p53 acetylation at K373/382 is assessed by Western blotting using acetylation-specific antibodies. Apoptosis is assessed by measuring caspase activity or by Annexin V staining. Cell viability and proliferation are measured using MTT or CellTiter-Glo assays. |
| Animal Protocol |
Animal/Disease Models: Balb/c nude mice (18-20 g; 6-8 weeks old) with MES-SA cells[1]
Doses: 2 mg/kg Route of Administration: Intraperitoneally injected; for 3 weeks, except on weekends. Experimental Results: Inhibited cancer growth in vivo. For in vivo studies, tumor xenograft models would be used. SIRT7 inhibitor 97491 would be administered via appropriate routes at doses determined from pharmacokinetic studies. Tumor growth would be monitored, and tumors would be collected for analysis of p53 acetylation, apoptosis markers, and SIRT7 inhibition. However, specific in vivo protocols for SIRT7 inhibitor 97491 have not been detailed in the available literature. |
| ADME/Pharmacokinetics |
SIRT7 inhibitor 97491 is soluble in DMSO. Storage is recommended at 4°C protected from light; in solvent, storage at -80°C for 6 months or -20°C for 1 month is recommended. Further detailed PK parameters including half-life, oral bioavailability, and tissue distribution would be required for in vivo studies. The compound is for research use only and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Toxicological data for SIRT7 inhibitor 97491 have not been extensively reported. In cell-based assays, the compound inhibits MES-SA cell growth without harming HEK293 cells. As a research compound, it is intended for laboratory use only and is not for human or veterinary use. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
SIRT7 inhibitor 97491 is a potent SIRT7 inhibitor with an IC50 of 325 nM. It reduces SIRT7 deacetylase activity, increases p53 stability through acetylation at K373/382, and promotes apoptosis through the caspase pathway. The compound has antitumor activity and inhibits MES-SA cell growth without harming HEK293 cells. SIRT7 inhibitor 97491 is a research tool and is not approved for clinical use.
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| Molecular Formula |
C15H12CLN3O
|
|---|---|
| Molecular Weight |
285.728281974792
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| Exact Mass |
285.066
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| CAS # |
1807758-81-1
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| PubChem CID |
146018038
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
310
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1)C1=CN=C(NC2C=CC=C(C=2)N)O1
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| InChi Key |
RMRVZWMKRCLSFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12ClN3O/c16-11-6-4-10(5-7-11)14-9-18-15(20-14)19-13-3-1-2-12(17)8-13/h1-9H,17H2,(H,18,19)
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| Chemical Name |
3-N-[5-(4-chlorophenyl)-1,3-oxazol-2-yl]benzene-1,3-diamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~500 mg/mL (~1749.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (14.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 41.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10 mg/mL (35.00 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4998 mL | 17.4990 mL | 34.9981 mL | |
| 5 mM | 0.7000 mL | 3.4998 mL | 6.9996 mL | |
| 10 mM | 0.3500 mL | 1.7499 mL | 3.4998 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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