S2116 | LSD1 inhibitor | Probechem Biochemicals

Chemical Structure : S2116

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S2116 (S2116 hydrochloride)

货号: PC-23354Not For Human Use, Lab Use Only.

S2116 is a specific, brain penetrant inhibitor of lysine-specific demethylase 1 (LSD1, KDM1A) withIC50 of 0.74 uM.

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生物&药学活性

S2116 is a specific, brain penetrant inhibitor of lysine-specific demethylase 1 (LSD1, KDM1A) withIC50 of 0.74 uM.
S2116 prevented teratoma formation from hiPSCs transplanted into immunodeficient mice.
S2116 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.
S2116 significantly retarded the growth of T-ALL cells in xenotransplanted mice and prolonged the survival of recipients as monotherapy and in combination with dexamethasone.
S2116 could almost completely eradicate CNS leukemia.

物理化学性质&存储条件

分子量	437.92
分子式	C22H26ClF2N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Ethanone, 1-[(3S)-3-amino-1-pyrrolidinyl]-2-[[(1R,2S)-2-[3,5-difluoro-2-(phenylmethoxy)phenyl]cyclopropyl]amino]-, hydrochloride (1:1)

参考文献

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.

S2116 (S2116 hydrochloride)

生物&药学活性

物理化学性质&存储条件

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S2116 (S2116 hydrochloride)

生物&药学活性

物理化学性质&存储条件

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