Home Tools

S2157

Catalog No. T39799 CAS 2262488-39-9

Synonyms: S2157

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

S2157, CAS 2262488-39-9

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Biological Description

Chemical Properties

Storage & Solubility Information

Description	S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.
In vitro	S2157 demonstrates notable efficacy against T-cell acute lymphoblastic leukemia (T-ALL) cell lines, with IC 50 values ranging from 1.1 μM in the CEM cell line to 6.8 μM in the MOLT4 cell line[1]. At concentrations between 4-20 μM over a 72-hour period, S2157 modestly inhibits the proliferation of mitogen-activated normal T-lymphocytes[1]. Furthermore, treatment with S2157 at doses of 4-8 μM for 24 hours leads to the induction of apoptosis in T-ALL cells and the reduced expression of NOTCH3 and TAL1 proteins, crucial markers involved in the disease's progression[1]. This activity is evidenced by increased annexin-V reactivity in flow cytometry analyses and confirmed through Western blot analysis, respectively, indicating a dose- and time-dependent effect without influencing the cell cycle distribution[1].
In vivo	Administration of S2157 at a dosage of 50 mg/kg intraperitoneally (IP) three times a week for 28 days significantly reduces the size of subcutaneous tumors to less than 20% compared to untreated controls in Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice implanted with MOLT4 cells. Moreover, at dosages of 30 mg/kg or 50 mg/kg, administered twice a week for three weeks, S2157 almost entirely suppresses the growth of MOLT4 cells in the majority of NOD/SCID mice, though not in all cases. Furthermore, S2157 effectively eradicates Central Nervous System (CNS) leukemia in murine xenotransplanted models. In pharmacokinetic analysis on 8-week-old ICR mice given a single dose of 50 mg/kg IP, S2157 exhibits a half-life (T 1/2) of 0.88 hours, a maximum concentration (C_max) of 4.33 μM, and an area under the curve (AUC) of 5.75 μM·h.

Synonyms	S2157
Molecular Weight	451.94
Formula	C23H28ClF2N3O2
CAS No.	2262488-39-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

S2157 2262488-39-9 S-2157 S 2157 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.