GSK2879552 2HCl (1401966-69-5(free base))

SKU: orb1302876

Description

GSK2879552 is an oral, irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1) developed for cancer research. It has demonstrated antineoplastic activity in studies targeting acute myeloid leukemia (AML) and small cell lung cancer (SCLC) in both in vitro and in vivo models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1902123-72-1
• MW: 437.4
• Purity: ≥95% (May vary between batches)
• Formula: C₂₃H₃₀Cl₂N₂O₂
• SMILES: Cl.Cl.OC(=O)c1ccc(CN2CCC(CN[C@@H]3C[C@H]3c3ccccc3)CC2)cc1
• Target: Histone Demethylase
• Solubility: DMSO:4.38 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  LSD1:
• In Vivo:
  GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice
• In Vitro:
  GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min 1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM
• Cell Research:
  Viable cells are measured in Cell Counting Kit-8 (CCK8) assay. Briefly, cells are cultured in a 96-well plate overnight at a density of 5×103 cells per well and treated with the indicated concentrations of sorafenib (0 μM, 40 μM or 80 μM) for 24 h. Subsequently, the cells are incubated with 10 μL CCK8 for 60 min at 37°C, 5% CO2. The absorbance of optical density at 450 nm (A450) is determined with Varioskan Flash.

Storage & Handling

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

Alternative Names

LSD1, HistoneDemethylase, Histone Demethylase, GSK2879552 2HCl (1401966 69 5(free base)), GSK2879552 2HCl (1401966695(free base)), GSK-2879552 2HCl (1401966-69-5(free base)), GSK2879552 2HCl (1401966-69-5(free base))

Compound Identifiers

PubChem CID

121272425