927019-63-4

927019-63-4 structure

Name: LSD1 inhibitor-1
Chemical Name: 1,1'-[1,3-Propanediylbis(imino-3,1-propanediyl)]bis(2,3-dimethylguanidine)
CAS Number: 927019-63-4
Molecular Formula: C₁₅H₃₆N₈
Molecular Weight: 328.500
Create Date: 2020-01-11 18:23:25
Modify Date: 2024-01-21 06:23:22
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; significantly increases H3K4me1 and H3K4me2 dose-dependently from 0.25 uM to 10 uM, without affecting global H3K9me2 in HCT116 human colon carcinoma cells; 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.

Name	1,1'-[1,3-Propanediylbis(imino-3,1-propanediyl)]bis(2,3-dimethylguanidine)
Synonyms	1,1'-[1,3-Propanediylbis(imino-3,1-propanediyl)]bis(2,3-dimethylguanidine) Guanidine, N,N'''-[1,3-propanediylbis(imino-3,1-propanediyl)]bis[N',N''-dimethyl-

Description	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; significantly increases H3K4me1 and H3K4me2 dose-dependently from 0.25 uM to 10 uM, without affecting global H3K9me2 in HCT116 human colon carcinoma cells; 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.
References	References 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. View Related Products by Target Histone Demethylase