Chemical Structure : S2157
CAS No.:
2262488-38-8
S2157
Catalog No.: PC-23356Not For Human Use, Lab Use Only.
S2157 is a selective, brain-permeable inhibitor of lysine-specific demethylase 1 (LSD1, KDM1A) with IC50 of 0.89 uM, >200-fold selective over LSD2, MAO-A and MAO-B.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
S2157 is a selective, brain-permeable inhibitor of lysine-specific demethylase 1 (LSD1, KDM1A) with IC50 of 0.89 uM, >200-fold selective over LSD2, MAO-A and MAO-B.
S2157 prevented teratoma formation from hiPSCs transplanted into immunodeficient mice.
S2157 induced apoptosis in TCP-resistant T-ALL cells in vitro and in vivo by repressing transcription of the NOTCH3 and TAL1 genes through increased H3K9 methylation and reciprocal H3K27 deacetylation at superenhancer regions.
S2157 significantly retarded the growth of T-ALL cells in xenotransplanted mice and prolonged the survival of recipients as monotherapy and in combination with dexamethasone.
S2157 could almost completely eradicate CNS leukemia.
Physicochemical Properties
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M.Wt
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415.48
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Formula
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C23H27F2N3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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rel-2-[[(1R,2S)-2-[3,5-Difluoro-2-(phenylmethoxy)phenyl]cyclopropyl]amino]-1-(4-methyl-1-piperazinyl)ethanone
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References
1. Saito S, et al. Clin Cancer Res. 2019 Mar 1;25(5):1601-1611.
2. Osada N, et al. Oncotarget. 2018 Jan 8;9(5):6450-6462.
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