Chemical Structure : S2116
CAS No.:
2262489-89-2
S2116
(S2116 hydrochloride)
Catalog No.: 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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
437.92
|
|
Formula
|
C22H26ClF2N3O2
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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)
|
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.
Contact Us
sales@probechem.com
