hdacin5

HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor [inducing apoptosis, with potential antineoplastic (antitumor) and chemopreventive activities], inhibiting cell proliferation and regulating cell differentiation (IC50=0.0056 µM, 72 h) in murine erythroleukemia cells.

HDAC-IN-51 is an HDAC inhibitor.

HDAC-IN-52, a pyridine-containing HDAC inhibitor, effectively inhibits HDAC1, HDAC2, HDAC3, and HDAC10 with IC50 values of 0.189, 0.227, 0.440, and 0.446 μM, respectively. HDAC-IN-52 can be used in cancer research.

HDAC-IN-50, a potent, orally active inhibitor targeting both FGFR (Fibroblast Growth Factor Receptor) and HDAC (Histone Deacetylase), exhibits IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. This dual inhibitor induces apoptosis and cell cycle arrest at the G0/G1 phase while decreasing the expression of phosphorylated FGFR1 (pFGFR1), phosphorylated ERK (pERK), and phosphorylated STAT3 (pSTAT3), thus demonstrating anti-tumor activity.

HDAC-IN-53 is an orally active, selective inhibitor of HDAC1-3, with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. It exhibits no inhibitory effects on class II HDACs (HDAC4, 5, 6, 7, 9; IC50 >10 μM). The compound induces caspase-dependent apoptosis and significantly hampers the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice with MC38 colon cancer [1].

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

HDAC-IN-55(8j) is a small-molecule inhibitor that enhances E-cadherin expression and suppresses cancer cell proliferation [1].

HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage, arrests the cell cycle at the G2/M phase, and triggers the mitochondrial apoptotic pathway, leading to cell apoptosis [1].

HDAC-IN-58, a selective HDAC6 inhibitor, exhibits potent inhibitory activity with an IC50 of 2.06 nM, rendering it suitable for research into chronic neurodegenerative and psychiatric disorders [1].

HDAC-IN-56 ((S)-17b), an orally active inhibitor of class I histone deacetylase (HDAC), exhibits inhibitory constants (IC 50) of 56.0 ± 6.0 nM for HDAC1, 90.0 ± 5.9 nM for HDAC2, 422.2 ± 105.1 nM for HDAC3, and greater than 10,000 nM for HDAC4-11. This compound displays robust antitumor activity [1], marked by its ability to significantly elevate intracellular acetylhistone H3 and P21 levels, while also inducing G1 cell cycle arrest and apoptosis effectively.