OSM-S-106
Based on 1 Customer Validation
OSM-S-106 is a species-selective reaction hijacking pro-inhibitor targeting the cytosolic asparaginyl-tRNA synthetase (PfAsnRS) of Plasmodium falciparum. OSM-S-106 undergoes PfAsnRS-mediated reaction hijacking to form the Asn-OSM-S-106 adduct, which blocks the PfAsnRS catalytic cycle, inhibits protein translation, and activates the amino acid starvation response. OSM-S-106 is useful for research on malaria, PfAsnRS, and the reaction hijacking mechanism of aminoacyl-tRNA synthetases.
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- Pureté : 99.34%
- CAS No.: 2650846-59-4
- Formule: C12H10N4O2S2
- Masse moléculaire:306.36
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
PfAsnRS |
In Vitro
OSM-S-106 (72 h) inhibits the growth of Plasmodium falciparum 3D7 with an IC50 of 0.058 μM[1].
OSM-S-106 (0.85 nM-50 μM) inhibits Plasmodium berghei liver-stage development in HepG2-A16-CD81-EGFP cells with IC50 values of 0.25/0.42 μM[1].
OSM-S-106 (6 h pulse exposure) reduces the survival of the next life cycle of Cam3.II-rev Plasmodium falciparum, with an IC50 of 4.7 μM[1].
OSM-S-106 (1-10 μM; 3 h) forms Asn-OSM-S-106 adducts in Plasmodium falciparum 3D7 cultures; at 10 μM, minor glycine and alanine adducts are also detected[1].
OSM-S-106 (0.003-0.8 μM; 72 h) shows a 6.6-fold enhanced activity against Plasmodium falciparum with conditional downregulation of PfAsnRS; downregulation of PfNT4 increases sensitivity by approximately 3-fold, whereas downregulation of PfAlaRS, PfGlyRS, PfGDH3, or PfCA produces no corresponding differential sensitivity[1].
OSM-S-106 (508 nM; continuous drug pressure; 60 days) produces no recrudescent wells in the Dd2-B2 Plasmodium falciparum single-step resistance selection experiment, with a minimum inoculum for resistance (MIR) >2.4 × 108 parasites[1].
OSM-S-106 (0.85 nM-50 μM) exhibits cytotoxicity against HepG2 cells with IC50 values of 49.6/47.3 μM, corresponding to a selectivity index of >140 relative to its activity against the Plasmodium berghei liver stage[1].
OSM-S-106 (6 h) inhibits protein translation in Cam3.II-rev P. falciparum trophozoites with an IC50 of 0.51 μM[1].
OSM-S-106 (2.5 μM; 3 h) induces eIF2α phosphorylation in Cam3.II-rev Plasmodium falciparum to an extent comparable to known aminoacyl-tRNA synthetase inhibition conditions, supporting the activation of the amino acid starvation response[1].
OSM-S-106 (2.5 h; with or without E. coli tRNA) inhibits ATP consumption by recombinant wild-type PfAsnRS and PfAsnRSR487S in the presence of tRNA, with IC50 values of 7.3 and 26 μM, respectively; in the absence of tRNA, the IC50 values are both >500 μM[1].
OSM-S-106 (1 h; in the presence of E. coli tRNA) inhibits ATP consumption by recombinant PfAsnRS with an IC50 of 6.2 μM, whereas its IC50 against HsAsnRS is >100 μM[1].
OSM-S-106 (1 μM; 37°C; 5-60 min) exhibits t1/2 values of 395/619 min in human liver microsomes and 19.7/20.4 min in mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2650846-59-4
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Appearance Solid
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Masse moléculaire 306.36
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Formule C12H10N4O2S2
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Color White to off-white
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SMILES
NC1=C2C(C=C(C3=CC(S(N)(=O)=O)=CC=C3)S2)=NC=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (326.41 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 (stored under nitrogen). 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 (stored under nitrogen). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 (stored under nitrogen). 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 | 3.2641 mL | 16.3207 mL | 32.6413 mL | 81.6033 mL |
| 5 mM | 0.6528 mL | 3.2641 mL | 6.5283 mL | 16.3207 mL | |
| 10 mM | 0.3264 mL | 1.6321 mL | 3.2641 mL | 8.1603 mL | |
| 15 mM | 0.2176 mL | 1.0880 mL | 2.1761 mL | 5.4402 mL | |
| 20 mM | 0.1632 mL | 0.8160 mL | 1.6321 mL | 4.0802 mL | |
| 25 mM | 0.1306 mL | 0.6528 mL | 1.3057 mL | 3.2641 mL | |
| 30 mM | 0.1088 mL | 0.5440 mL | 1.0880 mL | 2.7201 mL | |
| 40 mM | 0.0816 mL | 0.4080 mL | 0.8160 mL | 2.0401 mL | |
| 50 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6321 mL | |
| 60 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3601 mL | |
| 80 mM | 0.0408 mL | 0.2040 mL | 0.4080 mL | 1.0200 mL | |
| 100 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8160 mL |
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