Molecular Weight: | 437.90 |
Formula: | C19H20ClN3O5S |
Purity: | ≥98% |
CAS#: | 1423715-09-6 |
Solubility: | DMSO up to 50 mM |
Chemical Name: | (E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide |
Storage: | Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year. |
Biological Activity:
HCI-2509 (also named as SP2509 or LSD1-C12) is a highly potent, specific, and reversible Lysine Specific Demethylase-1 (LSD1) inhibitor. It inhibits LSD1 in biochemical assay with an IC50 ~13 nM, and has no activity against monoamine oxidase proteins MAO-A and MAO-B (>300 µM). HCI-2509 is a non-competitive inhibitor to bind LSD1, changes its solution dynamics in a manner distinct from TCP. It has minimal inhibition of CYPs and hERG, shows cellular activity against several cancer cell lines including endometrial, breast, colorectal, pancreatic, and prostate cancer (IC50 ~0.3-2.5 µM). HCI-2509 displayed sing-agent efficacy in multiple xenograft models and had good PK/PD relationship by using tumor histone H3K4 and H3K9 methylation. HCI-2509 serves as a very useful chemical probe to study the target biology of LSD1.How to Use:In vitro: HCI-2509 was used at 1 µM in vitro.In vivo: HCI-2509 was administered through IP injection at 25-30 mg/kg once per day in xenografts models. Reference:SouthernBiotech/Goat Anti-Human Lambda-Alexa Fluor® 555/2070-32/1.0 mg
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