DS68591889
Based on 1 Customer Validation
DS68591889 is a selective and orally active phosphatidylserine synthase 1 (PTDSS1) inhibitor. DS68591889 has no inhibitory activity against PTDSS2. DS68591889 induces the phospholipid imbalance in a wide range of cancer cells. DS68591889 negatively regulates B cell receptor (BCR)-induced Ca2+ signaling and subsequent apoptotic cell death. DS68591889 can be used for the cancer research, such as B cell lymphoma.
For research use only. We do not sell to patients.
- Purity : 99.18%
- CAS No.: 2488609-21-6
- Formula: C29H21F5N4O5
- Molecular Weight:600.49
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Phospholipase Isoforms
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Biological Activity
Description
IC50 & Target
PTDSS1[1]
In Vitro
DS68591889 (0.1-1000 nM; 4-6 days) strongly suppresses the growth of malignant B cell lymphoma-derived lines[1].
DS68591889 (100 nM; 3 days) enhances BCR-induced Ca2+ signaling and cell apoptosis in Ramos cells1.
DS68591889 (100 nM; 3 days) increases IP1 production, changes the levels of PI4P and PI(4,5)P2, and affects the subcellular localization of related proteins in Ramos cells1.
DS68591889 (100 nM; 24 hours) increases the PIP level, and alters the phospholipid metabolism related to ORP5/8 and Nir2/3 and the BCR-induced Ca2+ response in Ramos cells1.
In HeLa cells, DS68591889 (10-1000 nM; 2 days) causes a substantial loss of phosphatidylserine (PS) and phosphatidylethanolamine (PE), along with a slight decrease in phosphatidylglycerol (PG) and sphingomyelin (SM) and an increase in phosphatidic acid (PA)[1].
In a panel of 47 human cancer cell lines, DS68591889 causes a reduction of PS levels in a wide range of cell lines. DS68591889 reduces the levels of major PS acyl-chain species such as C36:1-PS and C34:1-PS, whereas it slightly increased the level of C40:6-PS, which is mainly produced by PTDSS2. DS68591889 also causes a profound reduction of C36:1-PE and C34:1-PE, indicating substantial PE production from PS species by PS decarboxylase in mitochondria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Ramos cells
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Concentration:100 nM
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Incubation Time:3 days
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Result:Enhanced BCR-induced Ca2+ signaling and cell apoptosis.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NSG mice (6-week-old) with intravenous injection of Jeko-1-Luc cells[1].
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Dosage:10 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:Oral administration, once daily, for 21 days
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Result:Suppressed Jeko-1 cell engraftment in the bone marrow of mice with systemic spread1.
Chemical Information
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CAS No. 2488609-21-6
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Appearance Solid
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Molecular Weight 600.49
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Formula C29H21F5N4O5
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Color White to off-white
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SMILES
O=C1OC2=C(C3=NNC4=C3C(C5=CC=C(C=C5)OC6=CC=C(C(C)=C6)OC(F)(F)F)N(CC(F)(C)F)C4=O)C=CC=C2N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 200 mg/mL (333.06 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 (protect from light). 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 (protect from light). 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 (8.33 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 (protect from light). 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 | 1.6653 mL | 8.3265 mL | 16.6531 mL | 41.6327 mL |
| 5 mM | 0.3331 mL | 1.6653 mL | 3.3306 mL | 8.3265 mL | |
| 10 mM | 0.1665 mL | 0.8327 mL | 1.6653 mL | 4.1633 mL | |
| 15 mM | 0.1110 mL | 0.5551 mL | 1.1102 mL | 2.7755 mL | |
| 20 mM | 0.0833 mL | 0.4163 mL | 0.8327 mL | 2.0816 mL | |
| 25 mM | 0.0666 mL | 0.3331 mL | 0.6661 mL | 1.6653 mL | |
| 30 mM | 0.0555 mL | 0.2776 mL | 0.5551 mL | 1.3878 mL | |
| 40 mM | 0.0416 mL | 0.2082 mL | 0.4163 mL | 1.0408 mL | |
| 50 mM | 0.0333 mL | 0.1665 mL | 0.3331 mL | 0.8327 mL | |
| 60 mM | 0.0278 mL | 0.1388 mL | 0.2776 mL | 0.6939 mL | |
| 80 mM | 0.0208 mL | 0.1041 mL | 0.2082 mL | 0.5204 mL | |
| 100 mM | 0.0167 mL | 0.0833 mL | 0.1665 mL | 0.4163 mL |
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