Iadademstat dihydrochloride (C09-1140-256)

Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A ( KDM1A / LSD1 ) inhibitor.In VitroIadademstat 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoIadademstat reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:KDM1A/LSD1. Specification: 0.99 Molecular Formula: C15H24Cl2N2 Molecular Weight: 303.27 PubChem CID: 71664305 Isomeric SMILES: C1CC(CCC1N)N[C@@H]2C[C@H]2C3=CC=CC=C3.Cl.Cl