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Iadademstat dihydrochloride

CAS No. : 1431303-72-8

MCE 站：Iadademstat dihydrochloride

产品活性：Iadademstat (ORY-1001) dihydrochloride 是一种不可逆的选择性赖氨酸特异性脱甲基酶 1A (KDM1A/LSD1) 抑制剂。

研究领域：Epigenetics

作用靶点：Histone Demethylase

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.

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

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