S2116

CAT: 0804-HY-136522-01Size: 5 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-136522-01Size:5 mg

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24/48H Stock Items & 2 to 6 Weeks non Stock Items.

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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].

CAS Number

2262489-89-2

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/s2116.html

Purity

98.05

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C22H26ClF2N3O2

Molecular Weight

437.91

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

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