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Chemical Structure : LSD1 inhibitor-1
Catalog No.: PC-61644Not For Human Use, Lab Use Only.
LSD1 inhibitor-1 is a bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 uM in vitro.
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LSD1 inhibitor-1 is a bisguanidine polyamine analogue that exhibits noncompetitive and specific LSD1 inhibition, with 14.1% remaining LSD1 activity at 10 uM in vitro.
LSD1 inhibitor-1 significantly increases H3K4me1 and H3K4me2 dose-dependently from 0.25 uM to 10 uM, without affecting global H3K9me2 in HCT116 human colon carcinoma cells.
LSD1 inhibitor-1 induces reexpression of several epigenetically silenced genes including SFRP1, SFRP4, SFRP5, and GATA5 more effectively when compared with siRNA treatment, particularly in the case of SFRP4 and SFRP5.
| M.Wt | 328.5 | |
| Formula | C15H36N8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sharma SK, et al. J Med Chem. 2010 Jul 22;53(14):5197-212.
2. Huang Y, et al. Proc Natl Acad Sci U S A. 2007 May 8;104(19):8023-8.
3. Bi X, et al. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3229-32.
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