Histone Acetyltransferases

RUSKI-201 dihydrochloride is a potent and selective inhibitor of Hedgehog acyltransferase (Hhat), demonstrating an IC50 of 0.20 μM. This compound effectively blocks Hedgehog signaling in cells overexpressing Sonic Hedgehog (Shh) and inhibits the palmitoylation process essential for Hh function. RUSKI-201 dihydrochloride serves as a valuable chemical probe for investigating Hhat catalytic activity in cellular studies, providing insights into the mechanisms of Hedgehog signaling.

IMP-1575 is a potent inhibitor of Hedgehog acyltransferase (HHAT), demonstrating an IC50 value of 0.75 μM against purified HHAT. This compound is valuable for research focused on cancer, particularly in studies exploring the role of the Hedgehog signaling pathway in tumorigenesis. Its specificity and efficacy make it a significant tool for investigating HHAT-related biological processes and potential therapeutic applications.

RUSKI-201 is a specific inhibitor of Hedgehog acyltransferase (Hhat), exhibiting an IC50 of 0.20 μM. This compound effectively disrupts Hedgehog (Hh) signaling in cells that overexpress Sonic Hedgehog (Shh) and inhibits the palmitoylation of Hh. RUSKI-201 serves as a valuable chemical probe for investigating Hhat catalytic function and its role in cellular signaling pathways.

Naa50-IN-1 is a potent inhibitor of N-alpha-acetyltransferase 50 (Naa50), exhibiting an IC50 of 7 nM against the human enzyme. This compound shows selectivity for related acetyltransferases, Naa10 and Naa60. Naa50-IN-1 interacts with the substrate-binding pocket of Naa50, with its binding affinity augmented by the presence of AcCoA, making it a valuable tool for investigating the biological roles of protein acetylation. Research applications include studies on gene regulation and enzyme activity related to Naa50 and its substrates.