ST-539
Based on 1 Customer Validation
ST-539 is an orally active USP30 inhibitor that crosses the blood-brain barrier, with an IC50 of 0.37 μM. ST-539 blocks USP30-mediated removal of ubiquitin from Parkin substrates, induces Parkin-mediated mitophagy and apoptosis during mitochondrial stress, and inhibits the AKT/mTOR signaling pathway. ST-539 can be used for research on T-cell leukemia, Parkinson's disease, and colon adenocarcinoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.00%
- CAS No.: 1040754-67-3
- Formule: C30H31N3O4S
- Masse moléculaire:529.65
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[2]|
USP30 0.37 μM (IC50) |
In Vitro
ST-539 (1-3 μg/mL; 18 h) requires functional PINK1/Parkin to promote TOM20 ubiquitination and reduce TOM20 and NDP52 in HeLa-Parkin cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hela Parkin USP30 cells
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Concentration:10 µg/mL (ST-539); 5 µM Antimycin A + 5 µM Oligomycin (HY-N6782) (AO)
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Incubation Time:0, 3, 6 h (AO; ST-539)
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Result:Decreased AKT protein levels during AO exposure.
Reduced TOM20 and increased cleaved PARP, indicating resumed Parkin-mediated mitophagy and apoptosis in Hela Parkin USP30 cells.
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Cell Line:Hela Parkin USP30 cells
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Concentration:10 µg/mL
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Incubation Time:48 h
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Result:Inhibiting USP30 significantly promoted AKT/mTOR inhibitor-induced loss of viability in Hela Parkin USP30 cells.
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Cell Line:Jurkat T leukemia cells
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Concentration:41 ng/mL; 120 ng/mL; 370 ng/mL; 1.1 µg/mL; 3.3 µg/mL; 10 µg/mL
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Incubation Time:72 h
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Result:Significantly improved MK-2206 efficacy in inhibiting Jurkat T cell growth.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-last | AUC0-inf | MRT0-last | MRT0-inf |
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| Mice[4] | 25 mg/kg | i.p. | 1427 ng/mL | 1.33 h | 3.85 h | 4162 ng·h/mL | 4240 ng·h/mL | 3.86 h | 4.27 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[3]
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Dosage:100 μl of 5 mg/mL (0.5 mg per mouse)
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Administration:oral gavage; every other day
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Result:Tumor growth curve showed a significant reduction compared with controls.
Resulted in a twofold increase in the MG+ TMRM+ CD8+ T cell population in tumor-infiltrating lymphocytes.
Significantly increased granzyme B levels in CD8+ TILs from MC38 tumors.
Had no significant impact on tumor-associated CD4+ T cell mitochondrial activity; frequencies of regulatory T cells, macrophages, myeloid cells, and NK cells remained unchanged.
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Animal Model:mt-Keima transgenic reporter (both male and female)[4]
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Dosage:25 mg/kg/day
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Administration:i.p.; once daily; 5 total doses
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Result:In heart tissue, marked induction of the red mt-Keima signal occurred, consistent with augmented cardiac mitophagy.
Heart LC3-II/LC3-I ratio was increased compared with control hearts.
In liver, the mt-Keima signal did not change.
In hippocampus, mitophagic flux remained unchanged.
Echocardiographic analysis showed minimal differences in EF.
Cardiac output and LVPWs did not appear to be impacted.
Chemical Information
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CAS No. 1040754-67-3
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Appearance Solid
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Masse moléculaire 529.65
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Formule C30H31N3O4S
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Color White to off-white
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SMILES
O=C(NC1=C2C=CC=C(S(=O)(NC(C)(C)C)=O)C2=CC=C1)C(NC(C3=CC=CC=C3)=O)CC4=CC=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (188.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.44 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (291 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8880 mL | 9.4402 mL | 18.8804 mL | 47.2010 mL |
| 5 mM | 0.3776 mL | 1.8880 mL | 3.7761 mL | 9.4402 mL | |
| 10 mM | 0.1888 mL | 0.9440 mL | 1.8880 mL | 4.7201 mL | |
| 15 mM | 0.1259 mL | 0.6293 mL | 1.2587 mL | 3.1467 mL | |
| 20 mM | 0.0944 mL | 0.4720 mL | 0.9440 mL | 2.3600 mL | |
| 25 mM | 0.0755 mL | 0.3776 mL | 0.7552 mL | 1.8880 mL | |
| 30 mM | 0.0629 mL | 0.3147 mL | 0.6293 mL | 1.5734 mL | |
| 40 mM | 0.0472 mL | 0.2360 mL | 0.4720 mL | 1.1800 mL | |
| 50 mM | 0.0378 mL | 0.1888 mL | 0.3776 mL | 0.9440 mL | |
| 60 mM | 0.0315 mL | 0.1573 mL | 0.3147 mL | 0.7867 mL | |
| 80 mM | 0.0236 mL | 0.1180 mL | 0.2360 mL | 0.5900 mL | |
| 100 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.4720 mL |
ST-539 Related Classifications
HY-114383 Related Classifications
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