2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. S2157

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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S2157 Chemical Structure

S2157 Chemical Structure

CAS No. : 2262488-39-9

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Based on 1 publication(s) in Google Scholar

S2157 Related Antibodies

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Description

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[1].

IC50 & Target

LSD1[1]
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.

S2157 Related Antibodies

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 T1/2 of 0.88 hours, a Cmax 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 T1/2 of 0.88 hours, a Cmax of 4.33 μM and an AUC of 5.75 μM•h.
Molecular Weight

451.94

Formula

C23H28ClF2N3O2
CAS No.
Appearance

Solid

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]
Shipping

Room temperature in continental US; may vary elsewhere.
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 (221.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2127 mL 11.0634 mL 22.1268 mL
5 mM 0.4425 mL 2.2127 mL 4.4254 mL
View the 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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 2.2127 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

S21572262488-39-9S 2157S-2157Histone DemethylaseApoptosisN-alkylatedtranylcypromineTCPlysine-specificdemethylase1LSD1T-cellacutelymphoblasticleukemiaT-ALLNOTCH3TAL1H3K9H3K27deacetylationInhibitorinhibitorinhibit

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