Background
AS-8351 is a small-molecule inhibitor of lysine demethylase 5B (JARID1B or KDM5B), which demethylates Lys4 of histone H3. AS-8351 is also involved in cell fate decisions and is overexpressed in a variety of human cancers (1). Overexpression of JARID1B is seen in breast cancer and correlates with increased metastasis. AS-8351 treatment of breast cancer cells inhibited breast cancer cell proliferation and migration. Additionally, AS-8351 reversed epithelial-mesenchymal transition and decreased fatty acid synthase and ATP citrate lyase protein levels in breast cancer cells (2). JARID1B is overexpressed in Ewing sarcoma (EWS) and correlates with poor outcomes in EWS patients. Inhibition of JARID1B by AS-8351 in EWS cells reduced cell proliferation and increased apoptosis and cell cycle arrest. AS-8351 inhibited tumor growth in EWS mouse xenografts, suggesting a possible role for AS-8351 in the clinical treatment of this disease (3).
Molecular Formula
C17H13N3O2
Molecular Weight
291.3 g/mol
Purity
>98%
CAS
796-42-9
Solubility
Soluble in DMSO at 45 mg/mL, ethanol at 10 mg/mL, or DMF at 30 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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