hdac-8-in-1

MDK-7933 (HDAC8-IN-1) is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines. MDK-7933 shows antiproliferative effects toward several human lung cancer cell lines (A549, H1299, and CL1-5). HDAC8-IN-1 exhibits cytotoxicity against human lung CL1-5 cells without significant cytotoxicity for normal IMR-90 cells[1].

ROCK HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK HDAC. This compound suppresses ROCK1 2 (IC50: 254.9 nM, 58.18 nM) and HDAC1 2 3 6 8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

Tubulin HDAC-IN-3 (compound 12a) is a potent dual inhibitor of tubulin polymerization and HDAC1 8, with IC50 values of 5.4 μM for tubulin polymerization, and 0.155 and 0.177 μM for HDAC1 and HDAC8, respectively. It obstructs the cell cycle, triggers apoptosis, and suppresses colony formation [1].

HDAC-IN-62 (Compound 5), an HDAC inhibitor, exhibits IC50 values of 0.78, 1.0, and 1.2 μM for HDAC6, HDAC8, and HDAC11, respectively. This compound suppresses microglial activation via autophagy induction and reduces nitric oxide production, demonstrating anti-inflammatory and antidepressant properties. Additionally, HDAC-IN-62 has been shown to inhibit microglial activation in mouse brains [1].

HDAC-IN-67 (compound 27f) acts as an inhibitor of HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and triggers apoptosis, while also displaying antitumor activity [1].

AES-350 is a potent and orally active HDAC6 inhibitor (IC50 and Ki of 0.0244 μM and 0.035 μM, respectively), also exhibiting activity against HDAC-3, -8, and -11 in an enzymatic assay with IC50 values of 0.187 μM, 0.245 μM, and >1 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.