1. Epigenetics
    Apoptosis
  2. Histone Demethylase
    Apoptosis
  3. S2116

S2116 

Cat. No.: HY-136522
Handling Instructions

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.

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S2116 Chemical Structure

S2116 Chemical Structure

CAS No. : 2262489-89-2

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Description

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[1].

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].

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

S2116 (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].
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].

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 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h.
Molecular Weight

437.91

Formula

C₂₂H₂₆ClF₂N₃O₂

CAS No.

2262489-89-2

SMILES

FC1=CC(F)=C(OCC2=CC=CC=C2)C([[email protected]]3[[email protected]](NCC(N4C[[email protected]@H](N)CC4)=O)C3)=C1.[H]Cl

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

S2116S 2116S-2116Histone DemethylaseApoptosisN-alkylatedtranylcypromineTCPlysine-specificdemethylase1LSD1T-cellacutelymphoblasticleukemiaT-ALLNOTCH3TAL1H3K9H3K27deacetylationInhibitorinhibitorinhibit

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