1620401-83-3

Basic information

• Product Name: UNC0379 (trifluoroacetate)
• Synonyms: UNC0379 (trifluoroacetate)
• CAS NO: 1620401-83-3
• Molecular Formula: C25H36F3N5O4
• Molecular Weight: 527.5796496
• Mol File: 1620401-83-3.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• CAS DataBase Reference: UNC0379 (trifluoroacetate)(CAS DataBase Reference)
• NIST Chemistry Reference: UNC0379 (trifluoroacetate)(1620401-83-3)
• EPA Substance Registry System: UNC0379 (trifluoroacetate)(1620401-83-3)

Safety Data

• Hazardous Substances Data: 1620401-83-3(Hazardous Substances Data)

Usage

General Description

UNC0379 (trifluoroacetate) is a chemical compound with the potential to inhibit lysine specific demethylase 1 (LSD1), an enzyme involved in the regulation of gene expression. By inhibiting LSD1, UNC0379 has the ability to modulate the activity of histone proteins, leading to potential impacts on transcription regulation and cellular signaling pathways. This chemical has shown promise as a potential therapeutic agent in cancer treatment, particularly in the context of leukemia and certain solid tumors. Additionally, UNC0379 has been studied for its potential role in the differentiation of stem cells, making it a compound of interest in the field of regenerative medicine. However, further research is needed to fully understand its mechanisms of action and potential application in various disease settings.

Upstream product

• 71302-71-1 5-(pyrrolidin-1-yl)pentan-1-amine 
• 27631-29-4 2-chloro-6,7-dimethoxy-3H-quinazolin-4-one 
• 123-75-1 pyrrolidine 
• 76-05-1 trifluoroacetic acid 

Relevant articles and documents

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8

The lysine methyltransferase SETD8 is the only known methyltransferase that catalyzes monomethylation of histone H4 lysine 20 (H4K20). Monomethylation of H4K20 has been implicated in regulating diverse biological processes including the DNA damage response. In addition to H4K20, SETD8 monomethylates non-histone substrates including proliferating cell nuclear antigen (PCNA) and promotes carcinogenesis by deregulating PCNA expression. However, selective inhibitors of SETD8 are scarce. The only known selective inhibitor of SETD8 to date is nahuoic acid A, a marine natural product, which is competitive with the cofactor. Here, we report the discovery of the first substrate-competitive inhibitor of SETD8, UNC0379 (1). This small-molecule inhibitor is active in multiple biochemical assays. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies. Importantly, compound 1 is selective for SETD8 over 15 other methyltransferases. We also describe structure-activity relationships (SAR) of this series.