DDD85646
Based on 1 publication(s) in Google Scholar
DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nM; hNMT IC50=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis.
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- Pureza : 99.72%
- No. CAS: 1215010-55-1
- Fòrmula: C21H24Cl2N6O2S
- Peso molecular:495.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DDD85646
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Actividad biológica
Descripciòn
IC50 & Target
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Trypanosoma |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
2.8 μM
Compound: 1; MMV688180
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
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[PMID: 30647879] |
| MRC5 | EC50 |
0.002 μM
Compound: 1
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Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
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[PMID: 25412409] |
| MRC5 | EC50 |
0.3 μM
Compound: 1
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Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
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[PMID: 25412409] |
| MRC5 | EC50 |
0.4 μM
Compound: 1; DDD85646
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CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
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[PMID: 29125744] |
In Vitro
DDD85646 (50 nM) female NMRI mouse model showed significant antitrypanosomic activity[3].
DDD85646 (0-100 nM; 6, 24h) has a targeting effect in Trypanosoma brucei, and can effectively inhibit the N-myristyl transferase (TbNMT) of bloodstream type Trypanosoma Brucei, and this inhibition is directly related to the inhibition of proliferation of Trypanosoma Brucei[3].
DDD85646 has an IC50 value of 4.4 nM for L. donovani NMT and an EC50 value of 8µM for L. donovani extracellular amastigotes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DDD85646 (0-50 mg/kg; Oral administration; Twice a day; 4 days) kills Trypanosoma brucei by acting on TbNMT in T. b. brucei acute mouse model of HAT[3].
DDD85646 (50 mg/kg; Oral administration; Twice a day) shows significant antitrypanosomic activity in female NMRI mice models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:T. b. brucei acute mouse model of HAT[3]
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Dosage:0-50 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Cured all animals in the T. b. brucei acute mouse model of HAT at a minimal oral dose of 12.5 mg/kg (b.i.d. for 4 days)
Prevented 99% of T. b. brucei proliferation
Parasite numbers dropped below detectable levels within 12 hours
Chemical Information
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No. CAS 1215010-55-1
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Appearance Solid
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Peso molecular 495.43
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Fòrmula C21H24Cl2N6O2S
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Color Light yellow to green yellow
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SMILES
O=S(C1=C(Cl)C=C(C2=CC(N3CCNCC3)=NC=C2)C=C1Cl)(NC4=C(C)N(C)N=C4C)=O
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Synonyms
IMP-366
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep
STBD1 mediates the crosstalk between glycogen and lipid droplets in clear cell renal cell carcinoma. [Abstract]2025 Oct 15;44(10):116429. PMID: 41105508
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (201.84 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: ≥ 2.5 mg/mL (5.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Spinks D, et al. Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode. ChemMedChem. 2015;10(11):1821-1836. [Content Brief]
[2]. Kallemeijn WW, et al. Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases. Cell Chem Biol. 2019;26(6):892-900.e4. [Content Brief]
[3]. Frearson JA, et al. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature. 2010;464(7289):728-732. [Content Brief]
[4]. Paape D, et al. Using a non-image-based medium-throughput assay for screening compounds targeting N-myristoylation in intracellular Leishmania amastigotes. PLoS Negl Trop Dis. 2014 Dec 18;8(12):e3363. [Content Brief]
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 | 2.0184 mL | 10.0922 mL | 20.1845 mL | 50.4612 mL |
| 5 mM | 0.4037 mL | 2.0184 mL | 4.0369 mL | 10.0922 mL | |
| 10 mM | 0.2018 mL | 1.0092 mL | 2.0184 mL | 5.0461 mL | |
| 15 mM | 0.1346 mL | 0.6728 mL | 1.3456 mL | 3.3641 mL | |
| 20 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5231 mL | |
| 25 mM | 0.0807 mL | 0.4037 mL | 0.8074 mL | 2.0184 mL | |
| 30 mM | 0.0673 mL | 0.3364 mL | 0.6728 mL | 1.6820 mL | |
| 40 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2615 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4037 mL | 1.0092 mL | |
| 60 mM | 0.0336 mL | 0.1682 mL | 0.3364 mL | 0.8410 mL | |
| 80 mM | 0.0252 mL | 0.1262 mL | 0.2523 mL | 0.6308 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5046 mL |
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