ORY-1001 (RG-6016) 2HCl
Molecular Weight(MW): 303.27
ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.
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Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells.
Br J Haematol, 2017, doi: 10.1111/bjh.14983. ORY-1001 (RG-6016) 2HCl purchased from Selleck.
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Choose Selective Histone Demethylase Inhibitors
|Description||ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.|
In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells. 
|In vivo||In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. |
|In vitro||Water||61 mg/mL (201.14 mM)|
|DMSO||5 mg/mL (16.48 mM)|
|Ethanol||4 mg/mL warmed (13.18 mM)|
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C15H22N2 . 2HCl
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