HDAC6 Inhibitor

HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC₅₀s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.

HDAC6 ligand 10 is a ligand that selectively targets HDAC6, and it can be used to synthesize PROTAC HDAC6 degrader 11 (HY-152134), a PROTAC-based HDAC6 degrader. HDAC6 ligand 10 applies to leukemia research.

HDAC6-IN-72 is a HDAC6 zinc finger ubiquitin-binding domain (ZnF-UBD) inhibitor that inhibits the interaction between HDAC6 ZnF-UBD and ubiquitin with an IC₅₀ of 2.7 μM. HDAC6-IN-72 can be used for the research of breast cancer, colorectal cancer, multiple myeloma.

LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC₅₀s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.

LT-630 is a HDAC6 inhibitor. LT-630 ameliorates liver injury by reducing oxidative damage.

HDAC6-IN-81 is a potent selective HDAC6 inhibitor with an IC₅₀ of 1 nM. HDAC6-IN-81 exhibits selectivity over class I HDAC isoforms (HDAC1/2/3/8). HDAC6-IN-81 can be used for the research of cancer.

CM-444 is inhibitor for HDAC (IC₅₀ is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC₅₀ is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.

HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC₅₀ values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.

HDAC6-IN-68 is an HDAC6 PROTAC ligand. HDAC6-IN-68 can be used to synthesize PROTAC HDAC6 degrader 7 (HY-179421).

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC₅₀ of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.

HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC₅₀ of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models.

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.

HDAC-IN-89 is an inhibitor of HDAC1 (IC₅₀: 0.95 nM), HDAC2 (IC₅₀: 0.86 nM), HDAC3 (IC₅₀: 1.06 nM) and HDAC8 (IC₅₀: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity.

ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC₅₀s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model.

HDAC6-IN-40 (Compound I-6) is an inhibitor for HDAC6 with IC₅₀ of 0.029 μM.

Nicoxamat (N-Hydroxynicotinamide) is a HCV inhibitor as well as a selective HDAC6 inhibitor. Nicoxamat is applicable to research related to hepatitis C virus (HCV) infection.

HDAC6-IN-39 (Compound I-132) is an inhibitor for HDAC6 with IC₅₀ of 0.0096 μM.

HDAC6-IN-78 (Example 48) is a selective HDAC6 inhibitor with an IC₅₀ of 24 nM. HDAC6-IN-78 shows no activity against other HDAC isoforms.

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The K_i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC₅₀s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model.