Iadademstat (ORY-1001) 2HCl

For research use only.

Catalog No.S7795 Synonyms: RG-6016

7 publications

Iadademstat (ORY-1001) 2HCl Chemical Structure

CAS No. 1431326-61-2

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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Selleck's Iadademstat (ORY-1001) 2HCl has been cited by 7 publications

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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. Iadademstat (ORY-1001) 2HCl purchased from Selleck.

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

Biological Activity

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.
LSD1 [1]
20 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 MWnGeY5kfGmxbjDhd5NigQ>? NYHSOFViOTNiZHH5dy=> NX;FOmJnUW6mdXP0bY9vKG:oIHTp[oZmemWwdHnheIlwdiCxZjDoeY1idiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzd4V{e2WmIHHzJIFtfGW{YYTpc44hcW5ibX;ydIhwdG:peTDv[kBkd2yxbnnld{Bi\nSncjCxN{Bl[Xm|IHL5JG1igSCJcoXue4Ft\C2JaXXtd4Ehe3SjaX7pcoch[mG|ZXSgZZN{[Xl? MkHNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5MEK1OFIoRjJ4N{CyOVQzRC:jPh?=
THP1 M3HmOmZ2dmO2aX;uJIF{e2G7 MWGxN{Bl[Xm| NVPzUVlUUW6mdXP0bY9vKG:oIHTp[oZmemWwdHnheIlwdiCxZjDoeY1idiCWSGCxJINmdGy|IHHmeIVzKDF|IHThfZMh[nliY4n0c5NxcW5iYYPzZZk> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjdyMkW0Nkc,OjZ5MEK1OFI9N2F-
HCT116 M{fvdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NVHrTpNROiC3TR?= Mon6NVYhfG9iM{CgbJJ{ M2[3bmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjdDCyJJVOKGGodHXyJFE3KHSxIEOwJIhzeyCkeTDtbYNzd3Olb4DpZ{BidmGueYPpdy=> NEC0ZVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzPVkyPid-Mkm0N|k6OTZ:L3G+
PA1 NYD2UoNsS3m2b4TvfIlkcXS7IHHzd4F6 M2TzbFIhfU1? NIfMeYkyPiC2bzCzNEBpenN? NXewWGxIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEFzIHPlcIx{KGG2IEKgeW0h[W[2ZYKgNVYhfG9iM{CgbJJ{KGK7IH3pZ5Jwe2OxcHnjJIFv[Wy7c3nz NIW4R5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzPVkyPid-Mkm0N|k6OTZ:L3G+
F9 NGPSXY5EgXSxdH;4bYNqfHliYYPzZZk> MXuyJJVO M4GxOVE3KHSxIEOwJIhzew>? MoD1R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgSlkh[2WubIOgZZQhOiC3TTDh[pRmeiBzNjD0c{A{OCCqcoOgZpkhdWmlcn;zZ49xcWNiYX7hcJl{cXN? NITMNY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzPVkyPid-Mkm0N|k6OTZ:L3G+

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell number ; 

PubMed: 30568590     

Cell proliferation was determined in H1299, A549, and BEAS-2B cells in the presence of increasing concentrations of ORY-1001.

In vivo In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. [1]


Animal Research:


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  • Animal Models: Rodent MV(4;11) xenografts
  • Dosages: <0.020mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro Water 61 mg/mL (201.14 mM)
DMSO 5 mg/mL (16.48 mM)
Ethanol 4 mg/mL warmed (13.18 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 303.27

C15H22N. 2HCl

CAS No. 1431326-61-2
Storage powder
in solvent
Synonyms RG-6016
Smiles C1CC(CCC1N)NC2CC2C3=CC=CC=C3.Cl.Cl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID