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

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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Based on 1 publication(s) in Google Scholar

S2116 Related Antibodies

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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].

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

S2116 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

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].

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 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.
Appearance

Solid

Color

Off-white to light yellow

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
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 (228.36 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 2.2836 mL 11.4179 mL 22.8357 mL
5 mM 0.4567 mL 2.2836 mL 4.5671 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 2.2836 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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S2116 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:

S21162262489-89-2S 2116S-2116Histone DemethylaseApoptosisN-alkylatedtranylcypromineTCPlysine-specificdemethylase1LSD1T-cellacutelymphoblasticleukemiaT-ALLNOTCH3TAL1H3K9H3K27deacetylationInhibitorinhibitorinhibit

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