Art. -Nr.: HY-136523

S2157

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S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.

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Reinheit: 98.44%
CAS. Nr.: 2262488-39-9
Formel: C₂₃H₂₈ClF₂N₃O₂
Molecular Weight:451.94

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

S2157 Chemical Structure

CAS. Nr.: 2262488-39-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

LSD1^[1]

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

In Vitro

S2157 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].
S2157 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes^[1].
S2157 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

Normal T-lymphocytes
Concentration:

4, 8, 12, 16, 20 µM
Incubation Time:

For 72 hours
Result:

Modestly inhibited mitogen-activated normal T-lymphocytes.

Apoptosis Analysis^[1]

Cell Line:

T-cell acute lymphoblastic leukemia (T-ALL) cells
Concentration:

4, 6, 8 µM
Incubation Time:

For 24 hours
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.

Western Blot Analysis^[1]

Cell Line:

T-ALL cells
Concentration:

4, 6, 8 µM
Incubation Time:

For 24 hours
Result:

Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells.

In Vivo

S2157 (50 mg/kg; IP; 3 times a week; for 28 days) causes the size of subcutaneous tumors reduced to less than 20% of that in the untreated control^[1].
S2157 (50 mg/kg; IP) has a T_1/2 of 0.88 hours, a C_max of 4.33 μM and an AUC of 5.75 μM•h^[1].
S2157 (30 mg/kg or 50 mg/kg; twice a week for 3 weeks) almost completely suppressed the growth of MOLT4 cells in most but not all NOD/SCID mice with MOLT4 cells. S2157 eradicates CNS leukemia in murine xenotransplanted models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells^[1]
Dosage:

50 mg/kg
Administration:

IP; 3 times a week; for 28 days
Result:

The size of subcutaneous tumors reduced to less than 20% of that in the untreated control.

Animal Model:

8-week-old ICR mice^[1]
Dosage:

50 mg/kg (Pharmacokinetic Analysis)
Administration:

IP
Result:

Had a T_1/2 of 0.88 hours, a C_max of 4.33 μM and an AUC of 5.75 μM•h.

Chemical Information

CAS. Nr. 2262488-39-9
Appearance Solid
Molecular Weight 451.94
Formel C₂₃H₂₈ClF₂N₃O₂
Color White to off-white
SMILES

[H]Cl.CN1CCN(C(CN[C@H]2[C@H](C3=CC(F)=CC(F)=C3OCC4=CC=CC=C4)C2)=O)CC1.[Relative stereochemistry]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (221.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2127 mL

11.0634 mL

22.1268 mL

5 mM

0.4425 mL

2.2127 mL

4.4254 mL

10 mM

0.2213 mL

1.1063 mL

2.2127 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shiori Saito, et al. Eradication of Central Nervous System Leukemia of T-Cell Origin With a Brain-Permeable LSD1 Inhibitor. Clin Cancer Res. 2019 Mar 1;25(5):1601-1611. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2127 mL	11.0634 mL	22.1268 mL	55.3171 mL
	5 mM	0.4425 mL	2.2127 mL	4.4254 mL	11.0634 mL
	10 mM	0.2213 mL	1.1063 mL	2.2127 mL	5.5317 mL
	15 mM	0.1475 mL	0.7376 mL	1.4751 mL	3.6878 mL
	20 mM	0.1106 mL	0.5532 mL	1.1063 mL	2.7659 mL
	25 mM	0.0885 mL	0.4425 mL	0.8851 mL	2.2127 mL
	30 mM	0.0738 mL	0.3688 mL	0.7376 mL	1.8439 mL
	40 mM	0.0553 mL	0.2766 mL	0.5532 mL	1.3829 mL
	50 mM	0.0443 mL	0.2213 mL	0.4425 mL	1.1063 mL
	60 mM	0.0369 mL	0.1844 mL	0.3688 mL	0.9220 mL
	80 mM	0.0277 mL	0.1383 mL	0.2766 mL	0.6915 mL
	100 mM	0.0221 mL	0.1106 mL	0.2213 mL	0.5532 mL

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S2157

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

S2157

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

S2157 Related Classifications

HY-136523 Related Classifications