2055397-18-5

Basic information

• Product Name: MOZ-IN-3
• Synonyms: MOZ-IN-3
• CAS NO: 2055397-18-5
• Molecular Formula: C20H17FN2O3S
• Molecular Weight: 384.4239832
• EINECS: -0
• Mol File: 2055397-18-5.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• Density: 1.307±0.06 g/cm3(Predicted)
• PKA: 7.15±0.25(Predicted)
• CAS DataBase Reference: MOZ-IN-3(CAS DataBase Reference)
• NIST Chemistry Reference: MOZ-IN-3(2055397-18-5)
• EPA Substance Registry System: MOZ-IN-3(2055397-18-5)

Safety Data

• Hazardous Substances Data: 2055397-18-5(Hazardous Substances Data)

Usage

Description

MOZ-IN-3 is an inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ) and KAT6B/MORF, characterized by its high potency and selectivity for these specific targets.

Uses

Used in Pharmaceutical Research and Development:
MOZ-IN-3 is used as a research tool for studying the role of KAT6A and KAT6B in various biological processes. Its selectivity and potency make it a valuable compound for investigating the mechanisms of action and potential therapeutic applications related to these lysine acetyltransferases.
Used in Cancer Research:
MOZ-IN-3 is used as a potential therapeutic agent in cancer research, given its ability to inhibit the proliferation of certain cancer cells, such as EMRK1184 lymphoma cells. Its mechanism of action, which includes inducing cell cycle arrest and cellular senescence without causing DNA damage, apoptosis, or necrosis, makes it a promising candidate for further exploration in oncology.
Used in Epigenetic Studies:
MOZ-IN-3 is utilized in epigenetic research to understand the effects of modulating histone acetylation, particularly at specific lysine residues. Its ability to decrease global levels of acetylated histone H3 lysine 14 (H3K14Ac) and reduce H3K9Ac levels at the transcription start sites of certain genes highlights its potential in exploring the epigenetic regulation of gene expression.

Upstream product

• 51437-00-4 5-bromo-2-fluorotoluene 
• 98-09-9 benzenesulfonyl chloride 
• 80-17-1 benzenesufonyl hydrazide 
• 98-80-6 phenylboronic acid 

Relevant articles and documents

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A

A high-throughput screen for inhibitors of the histone acetyltransferase, KAT6A, led to identification of an aryl sulfonohydrazide derivative (CTX-0124143) that inhibited KAT6A with an IC50 of 1.0 μM. Elaboration of the structure-activity relationship and medicinal chemistry optimization led to the discovery of WM-8014 (97), a highly potent inhibitor of KAT6A (IC50 = 0.008 μM). WM-8014 competes with acetyl-CoA (Ac-CoA), and X-ray crystallographic analysis demonstrated binding to the Ac-CoA binding site. Through inhibition of KAT6A activity, WM-8014 induces cellular senescence and represents a unique pharmacological tool.

ARYL SULFONOHYDRAZIDES

Compound of formula (I) wherein A is selected from (i), where RF1 is H or F; (ii); (iii) a N-containing C6 heteroaryl group; and B is (B), where X1 is either CRF2 or N, where RF2 is H or F; X2 is either CR3 or N, where R3 is selected from H, Me, CI, F OMe; X3 is either CH or N; X4 is either CRF3 or N, where RF3 is H or F; where only one or two of X1, X2, X3 and X4 may be N; and R4 is selected from I, optionally substituted phenyl, optionally substituted C5-6 heteroaryl; optionally substituted C1-6 aIkyI and optionally substituted C1-6 alkoxy, which are useful in the treatment of a condition ameliorated by the inhibition of MOZ.