2262488-39-9
Chemical Structure
S2157
- CAS No.: 2262488-39-9
- Formula:C23H28ClF2N3O2
- Molecular Weight:451.94
IUPAC Name: 2-(((1R,2S)-2-(2-(benzyloxy)-3,5-difluorophenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)ethan-1-one hydrochloride
InChIKey: PUXYOFXCUCMFSQ-OZYANKIXSA-N
SMILES: [H]Cl.CN1CCN(C(CN[C@H]2[C@H](C3=CC(F)=CC(F)=C3OCC4=CC=CC=C4)C2)=O)CC1.[Relative stereochemistry]
Biological Activity: 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].
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S2157 | 98.44% | 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. | ||||||||||||||||||||
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Keywords