1620401-82-2 Usage
Description
UNC0379, with the CAS number 1620401-82-2, is a selective inhibitor of the lysine methyltransferase SETD8, demonstrating its effectiveness over 15 other methyltransferases. It has shown promising results in inhibiting tumor growth and activating the p53 protein, a crucial tumor suppressor, in neuroblastoma cell lines such as SY5Y and NGP.
Uses
Used in Pharmaceutical Industry:
UNC0379 is used as an inhibitor for the lysine methyltransferase SETD8, which plays a significant role in the regulation of gene expression and cellular processes. Its selectivity over other methyltransferases makes it a valuable compound for targeted therapies in cancer treatment.
Used in Cancer Research:
In cancer research, UNC0379 is utilized to study the effects of SETD8 inhibition on tumor growth and the activation of the p53 protein. The compound has shown potential in decreasing tumor growth in ex-vivo tumorigenicity assays, particularly in neuroblastoma cell lines like SY5Y and NGP.
Used in Drug Development:
UNC0379 serves as a starting point for the development of new drugs targeting SETD8 in various cancer types. Its inhibitory properties and selectivity make it a promising candidate for further research and potential clinical applications in cancer treatment.
Used in Molecular Biology:
As a selective inhibitor of SETD8, UNC0379 is employed in molecular biology to investigate the role of this enzyme in gene regulation and its potential as a therapeutic target. Understanding the effects of SETD8 inhibition can provide insights into the development of targeted therapies for cancer and other diseases.
References
1) Ma et al. (2014), Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8; J. Med. Chem. 57 6822
2) Veschi et al. (2017), Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma; Cancer Cell 31 50
Check Digit Verification of cas no
The CAS Registry Mumber 1620401-82-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,2,0,4,0 and 1 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1620401-82:
(9*1)+(8*6)+(7*2)+(6*0)+(5*4)+(4*0)+(3*1)+(2*8)+(1*2)=112
112 % 10 = 2
So 1620401-82-2 is a valid CAS Registry Number.
1620401-82-2Relevant articles and documents
Structure-activity relationship studies of SETD8 inhibitors
Ma, Anqi,Yu, Wenyu,Xiong, Yan,Butler, Kyle V.,Brown, Peter J.,Jin, Jian
, p. 1892 - 1898 (2014)
SETD8 (also known as SET8, PR-SET7, or KMT5A (lysine methyltransferase 5A)) is the only known lysine methyltransferase that catalyzes the monomethylation of histone H4 lysine 20 (H4K20). In addition to H4K20, SETD8 monomethylates non-histone substrates such as the tumor suppressor p53 and the proliferating cell nuclear antigen (PCNA). Because of its role in regulating diverse biological processes, SETD8 has been pursued as a potential therapeutic target. We recently reported the first substrate-competitive SETD8 inhibitor, UNC0379 (1), which is selective for SETD8 over 15 other methyltransferases. We characterized this inhibitor in a battery of biochemical and biophysical assays. Here we describe our comprehensive structure-activity relationship (SAR) studies of this chemical series. In addition to 2- and 4-substituents, we extensively explored 6- and 7-substituents of the quinazoline scaffold. These SAR studies led to the discovery of several new compounds, which displayed similar potencies as compound 1 and interesting SAR trends. This journal is
