SP2509

SKU: orb1226307

Description

SP2509 is a potent, selective histone demethylase LSD1 (KDM1A) inhibitor with IC50 of 13 nM, shows no activity against MAOA, MAOB, LDH and glucose oxidase; inhibits the colony growth of OCI-AML3 significantly more than of the other AML cell-types, induces more apoptosis of AML cells expressing mutant NPM1 than mixed-lineage leukemia fusion oncoproteins; significantly improves the survival of immune-depleted mice model of AML, SP2509 is synergistically lethal against cultured and primary AML blasts combined with panobinostat.

Key Properties

• CAS Number: 1423715-09-6
• MW: 437.8972
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₀ClN₃O₅S
• SMILES: O=C(N/N=C(C1=CC(Cl)=CC=C1O)\C)C2=CC=CC(S(=O)(N3CCOCC3)=O)=C2
• Target: Histone Demethylase
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vivo:
  Treatment with SP2509 (25 mg/kg) and/or PS (5 mg/kg) significantly enhances PS-mediated loss of viability of CD34+ primary AML cells and improves the survival of mice bearing AML xenografts and primagrafts.
• In Vitro:
  SP2509 (250, 500, 1000 nM) inhibits LSD1 activity, depletes colony growth and induces apoptosis and cell death of cultured human acute myeloid leukemia cells, and increases H3K4Me3 on the promoters of p57 Kip, KLF4, and p21 and induces mRNA expression of p57Kip, KLF4 and p21 in AML cells. SP2509 (250, 1000 nM) induces features of morphologic differentiation of cultured and primary AML cells. Besides, SP2509 in combination with PS exerts synergistic lethal activity against cultured and primary AML cells. SP2509 does not destabilize the CoREST-LSD1 interaction, and has no major destabilizing effect on the CRC. SP2509 (1 or 10 μM) induces cell death, but there are no morphological changes at a low concertation of 0.1 μM. SP2509 likewise interferes with the viability of medulloblastoma cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SP-2509

Quick Database Links

Gene Symbol

Histone Demethylase