ORY-1001 (RG-6016) - LSD1 Inhibitor. CAS# 1431326-61-2 430 Structure and allosteric effects of

Structure and allosteric effects of low-molecular- weight activators on the protein kinase PDK1

InChi: InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4

InChi: InChI=1S/C24H32N6O3/c1-3-25-24(31)26-18-6-4-17(5-7-18)22-27-21-12-29(19-14-33-15-19)9-8-20(21)23(28-22)30-10-11-32-13-16(30)2/h4-7

72(4):897-907

ORY-1001 (RG-6016) - LSD1 Inhibitor. CAS# 1431326-61-2 430 Structure and allosteric effects ofORY 1001, CAS No. 1431326 61 2, is a highly potent and selective inhibitor of Lysine Specific Demethylase 1 (LSD1) with IC50 <20 nM. It is highly selective over related enzymes such as MAO A B. ORY 1001 affects AML stem cells, a sub population of cancer cells that has been proposed to be responsible for frequent relapses of the disease. It significantly reduces tumor cell load and increases survival time in mouse models of Acute Lymphoblastic