GSK-2879552

SKU: orb1226359

Description

A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM; shows good selectivity against LSD2, MAO-A, MAO-B, D-amino acid oxidase and LoxL2; exhibits growth inhibition (EC50=2-240 nM) in sensitive cell lines; orally bioavailable.Lung Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 1401966-69-5
• MW: 364.4806
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₈N₂O₂
• SMILES: O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1
• Target: Histone Demethylase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: NCI-H526 and NCI-H1417 xenografts. Dosage: 1.5 mg/kg. Administration: PO daily for 25-35 days. Result: There was 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 demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.
• In Vitro:
  Cell Proliferation Assay. Cell line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration: 0-10000 nM. Incubation time: 6 days. Result: Inhibited cell proliferation. RT-PCR. Cell line: Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration: 0, 1, 2 μM. Incubation time: 24 h. Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

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

GSK2879552

Quick Database Links

Gene Symbol

Histone Demethylase