SMER 3 (Synonyms: SCFMET30 Inhibitor, MET30 Antagonist) |
Catalog No.GC15492
One-Click Copy Product Info
|
SMER 3 is a small-molecule compound that selectively inhibits the SCFMet30 ubiquitin E3 ligase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67200-34-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
SMER 3 is a small-molecule compound that selectively inhibits the SCFMet30 ubiquitin E3 ligase. By directly binding to the F-box protein Met30, SMER 3 disrupts the interaction between Met30 and Skp1, thereby specifically inhibiting the activity of the SCFMet30 ubiquitin ligase without affecting the function of other SCF complexes, such as SCFCdc4[1].
In vitro, pretreatment of HeLa, A549, and HT-29 cells with SMER 3 (2.5–50μM) for 24 hours significantly enhances oxidative stress and induces cell death in cancer cells by promoting hydrogen peroxide (H₂O₂) accumulation and mitochondrial dysfunction[2]. Treatment of human umbilical vein endothelial cells (HUVECs) with SMER 3 (0.1–1μM) for 3–6 hours specifically inhibits the activity of SCF-family E3 ubiquitin ligases, markedly increasing the stability of the glycolytic key protein PFKFB3 and reducing its ubiquitination level[3].
References:
[1] Aghajan M, Jonai N, Flick K, et al. Chemical genetics screen for enhancers of rapamycin identifies a specific inhibitor of an SCF family E3 ubiquitin ligase. Nat Biotechnol. 2010 Jul;28(7):738-42.
[2] Hao Y, Langford TF, Moon SJ, et al. Screening compound libraries for H2O2-mediated cancer therapeutics using a peroxiredoxin-based sensor. Cell Chem Biol. 2022 Apr 21;29(4):625-635.e3.
[3] Boscaro C, Carotti M, Albiero M, et al. Non-genomic mechanisms in the estrogen regulation of glycolytic protein levels in endothelial cells. FASEB J. 2020 Sep;34(9):12768-12784.
| Cell experiment [1]: | |
Cell lines | HeLa, A549 (human lung adenocarcinoma), and HT-29 (human colon adenocarcinoma) cells |
Preparation Method | The three cancer cell lines were maintained in their respective standard media (DMEM for HeLa/A549, McCoy's 5A for HT-29) supplemented with 10% FBS at 37°C, 5% CO₂. Cells were treated with various concentrations of SMER 3(2.5-50μM) for 24 hours. |
Reaction Conditions | 5-50μM; 24h |
Applications | SMER 3 exhibited differential cytotoxicity across the cell lines. HT-29 cells, which displayed higher baseline mitochondrial oxidative stress (evidenced by a greater fraction of oxidized Prx3 dimer under basal conditions), showed the highest sensitivity to SMER 3 treatment. A549 cells, known to have hyperactive Nrf2 antioxidant signaling, exhibited the least sensitivity. |
References: | |
| Cas No. | 67200-34-4 | SDF | |
| Synonyms | SCFMET30 Inhibitor, MET30 Antagonist | ||
| Chemical Name | 9H-indeno[1,2-b][1,2,5]oxadiazolo[3,4-e]pyrazin-9-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2C3=NC4=NON=C4N=C31 | ||
| Formula | C11H4N4O2 | M.Wt | 224.18 |
| Solubility | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.4607 mL | 22.3035 mL | 44.607 mL |
| 5 mM | 892.1 μL | 4.4607 mL | 8.9214 mL |
| 10 mM | 446.1 μL | 2.2304 mL | 4.4607 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)