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Medchemexpress LLC S2116 | 2262489-89-2 | 98.1% | 437.91 | 50 MG
Supplier: Medchemexpress LLC HY13652250MG
S2116 is an N-alkylated tranylcypromine (TCP) derivative and a potent lysine-specific demethylase 1 (LSD1) inhibitor. It enhances H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 can induce apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by suppressing the transcription of NOTCH3 and TAL1 genes and has been shown to significantly slow the growth of T-ALL cells in xenotransplanted mice.
- Potent lysine-specific demethylase 1 (LSD1) inhibitor
- Effective for T-ALL cell lines with IC50 values ranging from 1.1 μM to 6.8 μM
- Induces apoptosis and down-regulates NOTCH3 and TAL1 protein expression in T-ALL cells
- Significantly reduces subcutaneous tumor size in xenotransplanted mice
- Exhibits favorable pharmacokinetic properties in mice with a T1/2 of 3.76 hours
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