You are here:Home-Chemical Inhibitors & Agonists-Epigenetics-Histone Demethylase-S2116
S2116

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.

Packing Price Stock Quantity
50 mg Get quote
100 mg Get quote
250 mg Get quote

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.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: