For research use only. Not for therapeutic Use.
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
IC50 Value: 5.27 uM
Target: hLSD1
CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).
| Catalog Number | I046387 |
| CAS Number | 2070015-03-9 |
| Synonyms | methyl 3-[4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl]-5-[(4-carbamimidoylpiperazin-1-yl)methyl]benzoate;trihydrochloride |
| Molecular Formula | C27H37Cl3N8O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H34N8O4.3ClH/c1-39-26(38)22-15-18(17-32-6-8-35(9-7-32)27(30)31)14-21(16-22)25(37)34-12-10-33(11-13-34)24(36)20-4-2-19(3-5-20)23(28)29;;;/h2-5,14-16H,6-13,17H2,1H3,(H3,28,29)(H3,30,31);3*1H |
| InChIKey | RIIIVYLDVVJOFM-UHFFFAOYSA-N |
| 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 |
| Reference | [1]. Wang J, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer Res. 2011 Dec 1;71(23):7238-49. |
