Description
Lysine-specific Demethylase Inhibitor (1C) is a lysine-specific demethylase inhibitor. Lysine-specific demethylase 1 (LSD1) is the first of several protein lysine demethylases identified. Through a FAD-dependent oxidative reaction, LSD1 could specifically remove histone H3K4me2 to H3K4me1 or H3K4me0. When forming a complex with androgen receptor, LSD1 alters its substrates to H3K9me2. The LSD1 complex regulates a coordinated histone modification switch via enzymatic activities and histone modification readers. In vitro: Lysine-specific Demethylase Inhibitor (1C) was identified as a bisguanidine polyamine analogue exhibiting noncompetitive and specific LSD1 inhibition, with 14.1% in vitro LSD1 activity at 10 μM. Lysine-specific Demethylase Inhibitor (1C) at 0.25 μM to 10 μM could significantly and dose-dependently increase methylation at the histone 3 lysine 4 chromatin mark, H3K4me1 and H3K4me2, without affecting global H3K9me2 levels in HCT116 human colon carcinoma cells. Lysine-specific Demethylase Inhibitor (1C) could also induce expression of several epigenetically silenced genes, such as SFRP1, SFRP4, SFRP5, and GATA5, particularly in the case of SFRP4 and SFRP5 . In vivo: Currently, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 927019-63-4
Molecular Weight: 328.50
Formula: C15H36N8
Chemical Name: (E)-N'-(3-{[3-({3-[(E)-N',N''-dimethylcarbamimidamido]propyl}amino)propyl]amino}propyl)-N,N''-dimethylguanidine
Smiles: C/N=C(/NCCCNCCCNCCCN/C(/NC)=N/C)\NC
InChiKey: UECHIPVWNJCQJH-UHFFFAOYSA-N
InChi: InChI=1S/C15H36N8/c1-16-14(17-2)22-12-6-10-20-8-5-9-21-11-7-13-23-15(18-3)19-4/h20-21H,5-13H2,1-4H3,(H2,16,17,22)(H2,18,19,23)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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