SP2509 (HCI-2509)

Description: SP2509 (HCI2509) is a novel, potent and selective histone demethylase LSD1 (KDM1A) antagonist with antineoplastic activity. It inhibits LSD1 with an IC50 of 13nM, and shows no/little activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP-2509 exhibits excellent antiproliferative activity and high in vivo antitumor efficacy. It showed high actitivity on human AML cells. Treatment with the novel LSD1 antagonist SP2509 attenuated the binding of LSD1 with the corepressor CoREST, increased the permissive H3K4Me3 mark on the target gene promoters, and increased the levels of p21, p27 and CCAAT/enhancer binding protein alpha in cultured AML cells.

References: Leukemia. 2014 Nov; 28(11):2155-64.

SP 2509; SP-2509; SP2509.

Chemical Name: (E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide.

InChi Key: NKUDGJUBIVEDTF-FYJGNVAPSA-N

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+

SMILES Code: O=C(N/N=C(C1=CC(Cl)=CC=C1O)\C)C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2