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MedChemExpress - Model Iadademstat dihydrochloride -1431303-72-8

Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

Iadademstat dihydrochloride

MCE China：Iadademstat dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-12782T

CAS：1431303-72-8

Synonyms：ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

Purity：99.98%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

In Vitro：Iadademstat dihydrochloride is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. Iadademstat has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. Iadademstat provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to Iadademstat[1].

In Vivo：Iadademstat reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL[1].

IC50 & Target：KDM1A/LSD1[1] Cellular Effect Cell Line Type Value Description References

References：

[1]. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9. [Content Brief]

[2]. Tamara Maes, et al. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia. Cancer Cell. 2018 Mar 12;33(3):495-511.e12. [Content Brief]

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MedChemExpress - Model Iadademstat dihydrochloride -1431303-72-8

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Iadademstat dihydrochloride