S2116
Based on 1 Customer Validation
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
For research use only. We do not sell to patients.
- Purity : 98.05%
- CAS No.: 2262489-89-2
- Formula: C22H26ClF2N3O2
- Molecular Weight:437.91
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
LSD1[1]
In Vitro
S2116 is particularly effective for T-ALL cell lines with the IC50 values between 1.1 µM for human T-ALL cell lines CEM and 6.8 µM for MOLT4[1].
S2116 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes[1].
S2116 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-ALL cells[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:Normal T-lymphocytes
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Concentration:4, 8, 12, 16, 20 µM
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Incubation Time:For 72 hours
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Result:Modestly inhibited mitogen-activated normal T-lymphocytes.
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Cell Line:T-cell acute lymphoblastic leukemia (T-ALL) cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Induced apoptosis, as evidenced by increased annexin-V reactivity on flow cytometry in T-ALL cells in a dose- and time-dependent manner without affecting cell cycle distribution.
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Cell Line:T-ALL cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells.
In Vivo
S2116 (50 mg/kg; IP) has a T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells[1]
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Dosage:50 mg/kg
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Administration:IP; 3 times a week; for 28 days
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Result:The size of subcutaneous tumors reduced to less than 20% of that in the untreated control.
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Animal Model:8-week-old ICR mice[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:IP
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Result:Had a T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h.
Chemical Information
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CAS No. 2262489-89-2
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Appearance Solid
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Molecular Weight 437.91
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Formula C22H26ClF2N3O2
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Color Off-white to light yellow
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SMILES
FC1=CC(F)=C(OCC2=CC=CC=C2)C([C@H]3[C@H](NCC(N4C[C@@H](N)CC4)=O)C3)=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (228.36 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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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
Purity & Documentation
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Data Sheet (277 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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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 (sealed storage, away from moisture). 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 | 2.2836 mL | 11.4179 mL | 22.8357 mL | 57.0894 mL |
| 5 mM | 0.4567 mL | 2.2836 mL | 4.5671 mL | 11.4179 mL | |
| 10 mM | 0.2284 mL | 1.1418 mL | 2.2836 mL | 5.7089 mL | |
| 15 mM | 0.1522 mL | 0.7612 mL | 1.5224 mL | 3.8060 mL | |
| 20 mM | 0.1142 mL | 0.5709 mL | 1.1418 mL | 2.8545 mL | |
| 25 mM | 0.0913 mL | 0.4567 mL | 0.9134 mL | 2.2836 mL | |
| 30 mM | 0.0761 mL | 0.3806 mL | 0.7612 mL | 1.9030 mL | |
| 40 mM | 0.0571 mL | 0.2854 mL | 0.5709 mL | 1.4272 mL | |
| 50 mM | 0.0457 mL | 0.2284 mL | 0.4567 mL | 1.1418 mL | |
| 60 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9515 mL | |
| 80 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7136 mL | |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2284 mL | 0.5709 mL |
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