hdacin7

HDAC-IN-7, an analogue of Tucidinostat (Chidamide), is a HDAC inhibitor. HDAC-IN-7 inhibits acetylation of histone protein H3 and induces apoptosis in human colon cancer cell lines[1].

HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.

HDAC-IN-76 (compound 6i), a histone deacetylase (HDAC) inhibitor, demonstrates robust antimalarial activity, particularly against the asexual blood stages of Plasmodium. The compound exhibits potent efficacy with IC 50 values of 30 nM and 98 nM against Pf3D7 (chloroquine drug-susceptible strain) and PfDd2 (chloroquine drug-resistant strain), respectively. Moreover, HDAC-IN-76 shows selective inhibition towards parasites, displaying IC 50 values of 7 nM and 9 nM against human HDAC1 and HDAC6, respectively, and effectively inhibits PfHDAC1.

HDAC-IN-78 (compound 66a) is an HDAC inhibitor utilized for cancer research.

HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.

HDAC-IN-75 (5d) is an inhibitor of HDAC, exhibiting IC50 values of 6.32 nM for HDAC6 and 1352 nM for HDAC1. Additionally, HDAC-IN-75 (5d) can restore photoreceptor function deficits in atp6v0e1–/– mutant zebrafish models.

HDAC-IN-72 (compound 7j), a potent inhibitor of HDAC1 (IC 50 =0.65 ± 0.07 μM), HDAC2 (IC 50 =0.78 ± 0.02 μM), and HDAC3 (IC 50 =1.70 ± 0.1 μM), exhibits significant antiproliferative properties. This compound is employed in breast cancer research [1].

HDAC-IN-73 (compound p-503), an effective HDAC inhibitor, exhibits IC 50 values of 0.17 and 0.49 µM for HDAC1 and HDAC6 respectively. This compound promotes apoptosis and arrests the cell cycle at the G2/M phase. Additionally, HDAC-IN-73 demonstrates anti-tumor activity.

HDAC-IN-74 (PA) is a dual inhibitor of HDAC and ribonucleotide reductase (RR), exhibiting IC50 values of 10.80 μM and 9.34 μM respectively for each enzyme. This compound is utilized in cancer research studies.