hat-in-1

HAT-IN-1, an inhibitor of HAT (histone acetyltransferase), is utilized in cancer research.

HAT-SIL-TG-1&AT, a hypoxia-activated prodrug, functions as a Janus tyrosine kinase (JAK) inhibitor demonstrating antitumor effects by inhibiting JAK-STAT signaling within tumor tissues. It also suppresses the proliferation of HEL cells and downregulates phosphorylated STAT3/5 in hypoxic conditions.

HAT-IN-8 (Compound 38), a blood-brain barrier-permeable inhibitor of Trypanosoma brucei with an EC50 of 0.18 μM, is utilized in the study of Human African trypanosomiasis [1].

NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].

20S Proteasome-IN-4 (Compound 7) is an orally active inhibitor of the 20S proteasome, selectively targeting the parasite form and demonstrating brain penetration capabilities. It exhibits a potent IC50 value of 6.3 nM against the T. b. brucei 20S proteasome, making it suitable for human African trypanosomiasis (HAT) research [1].

CBP p300-IN-16 (compound 1) is a potent inhibitor of EP300 CBP HAT, targeting HAT EP300 with an IC50 of 0.61 μM and LK2 H3K27 with an IC50 of 2.24 μM.