SP-2509

• CAT Number: I001637
• CAS Number: 1423715-09-6
• Molecular Formula: C₁₉H₂₀ClN₃O₅S
• Molecular Weight: 437.90
• Purity: ≥95%
• Synonyms: (E)-N/’-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide
• Target: Histone Demethylases
• Solubility: DMSO: ≥ 35 mg/mL
• Storage: Store at -20°C
• IC50: 13 nM
• IUPAC Name: N-[(E)-1-(5-chloro-2-hydroxyphenyl)ethylideneamino]-3-morpholin-4-ylsulfonylbenzamide
• InChI: 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+
• InChIKey: NKUDGJUBIVEDTF-FYJGNVAPSA-N
• SMILES: C/C(=N\NC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)/C3=C(C=CC(=C3)Cl)O

SP-2509（Cat No.:I001637）is a selective inhibitor of the histone methyltransferase DOT1L (disruptor of telomeric silencing 1-like), which is responsible for the methylation of histone H3 at lysine 79 (H3K79). By inhibiting DOT1L, SP-2509 disrupts the aberrant gene expression associated with various cancers, particularly those driven by MLL (Mixed-Lineage Leukemia) rearrangements. This compound has shown significant anti-cancer activity in preclinical models, demonstrating potential in treating hematologic malignancies and solid tumors. SP-2509’s unique mechanism highlights its promise as a targeted therapeutic agent for combating DOT1L-related oncogenic processes.

Reference

[1]. Fiskus W, et al. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64.