Iadademstat (ORY-1001) 2HCl

Catalog No.S7795 Batch:S779503

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Technical Data

Formula

C15H22N2 . 2HCl
Molecular Weight 303.27 CAS No. 1431326-61-2
Solubility (25°C)* In vitro Water 60 mg/mL (197.84 mM)
DMSO 6 mg/mL (19.78 mM)
Ethanol 1 mg/mL (3.29 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
Targets
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]
In vivo

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

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    NRK-52E cells

  • Concentrations

    10 μM

  • Incubation Time

    24 h

  • Method

    Cells treated with ORY-1001 (10 μM) for 24 h in the presence (vehicle) or TGF-β1.
Animal Study:

[1]
  • Animal Models

    Rodent MV(4;11) xenografts

  • Dosages

    <0.020mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Br J Haematol, 2017, doi: 10.1111/bjh.14983]

Selleck's Iadademstat (ORY-1001) 2HCl has been cited by 24 publications

Transposable elements-mediated recruitment of KDM1A epigenetically silences HNF4A expression to promote hepatocellular carcinoma [ Nat Commun, 2024, 15(1):5631] PubMed: 38965210
Potential role of lipophagy impairment for anticancer effects of glycolysis-suppressed pancreatic ductal adenocarcinoma cells [ Cell Death Discov, 2024, 10(1):166] PubMed: 38580661
MAF amplification licenses ERα through epigenetic remodelling to drive breast cancer metastasis [ Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y] PubMed: 37945904
Pharmacological inhibition of LSD1 suppresses growth of hepatocellular carcinoma by inducing GADD45B [ MedComm (2020), 2023, 4(3):e269] PubMed: 37250145
E3 ligase Trim35 inhibits LSD1 demethylase activity through K63-linked ubiquitination and enhances anti-tumor immunity in NSCLC [ Cell Rep, 2023, 10.1016/j.celrep.2023.113477] PubMed: 37979167
Targeting Lysine-Specific Demethylase 1 Rescues Major Histocompatibility Complex Class I Antigen Presentation and Overcomes Programmed Death-Ligand 1 Blockade Resistance in SCLC [ J Thorac Oncol, 2022, 17(8):1014-1031] PubMed: 35691495
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
Targeting histone demethylase LSD1 for treatment of deficits in autism mouse models [ Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8] PubMed: 35296809
Loss-of-function variants in the schizophrenia risk gene SETD1A alter neuronal network activity in human neurons through the cAMP/PKA pathway [ Cell Rep, 2022, 39(5):110790] PubMed: 35508131
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity [ J Enzyme Inhib Med Chem, 2022, 37(1):973-985] PubMed: 35317680

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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