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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[1].

Product Specifications

CAS Number

2262488-39-9

UNSPSC

12352005

Target

Apoptosis; Histone Demethylase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/s2157.html

Purity

98.44

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C23H28ClF2N3O2

Molecular Weight

451.94

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

KDM1/LSD1

Available Sizes

Frequently Asked Questions

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