SP-2509

Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4), resulting in transcriptional repression. SP-2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM). It has no effect on monoamine oxidases A and B. SP-2509 attenuates the binding of LSD1 to CoREST, allowing increased methylation of H3K4 and driving increased expression of p21, p27, and CCAAT/enhancer binding protein alpha in cultured acute myeloid leukemia (AML) cells. It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks. Co-treatment of SP2509 with the pan-HDAC inhibitor panobinostat (Cay-13280) synergistically kills AML cells in vitro and improves survival of mice engrafted with AML cells.Formal Name: 3-(4-morpholinylsulfonyl)-benzoic acid (2E)-2-[1-(5-chloro-2-hydroxyphenyl)ethylidene]hydrazide. CAS Number: 1423715-09-6. Synonyms: HCI-2509, LSD1 Inhibitor VII. Molecular Formula: C19H20ClN3O5S. Formula Weight: 437.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 25 mg/ml. lambdamax: 220, 284, 336 nm. SMILES: O=S(C1=CC(C(N/N=C(C)/C2=C(O)C=CC(Cl)=C2)=O)=CC=C1)(N3CCOCC3)=O. InChi Code: InChI=1S/C19H20ClN3O5S/c1-13(17-12-15(20)5-6-18(17)24)21-22-19(25)14-3-2-4-16(11-14)29(26,27)23-7-9-28-10-8-23/h2-6,11-12,24H,7-10H2,1H3,(H,22,25)/b21-13+. InChi Key: NKUDGJUBIVEDTF-FYJGNVAPSA-N.