CBB1007 hydrochloride

• Target:

  Others|||Histone Demethylase

• Related Pathways:

  Chromatin/Epigenetic|||Others

• Bioactivity:

  CBB1007 HCl is a cell-permeable amidino-guanidinium compound identified as a potent, reversible, and substrate-competitive inhibitor of LSD1 (IC50 = 5.27 ?M for hLSD1) . It effectively inhibits LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ? 5 ?M), without affecting H3K4Me3 and H3K9Me2 demethylation, nor the activities of LSD2 and JARID1A. Moreover, CBB1007 increases the levels of H3K4Me2 and H3K4Me (IC50 ? 5 ?M) and activates epigenetically suppressed genes CHRM4/M4-ArchR and SCN3A in F9 cells (IC50 ? 3.74 ?M) . It preferentially inhibits the growth of pluripotent tumors with minimal impact on non-pluripotent cancer or normal somatic cells (IC50 ? 100 ?M) .

• Smiles:

  COC(=O)C1=CC(=CC(=C1)C(=O)N2CCN(CC2)C(=O)C3=CC=C(C=C3)C(=N)N)CN4CCN(CC4)C(=N)N.Cl.Cl.Cl.Cl.Cl

• Molecular Formula:

  C27H39Cl5N8O4

• Molecular Weight:

  716.91

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2070014-96-7