hdac 6

HDAC6 degrader 9c is a small molecule histone deacetylase 6 (HDAC6) degrader that can be used to study cancer or other diseases.

BChE/HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.

TCS HDAC6 20b (HDAC6-IN-7) is a selective HDAC6 inhibitor that blocks the growth of breast cancer cells and may be used in the study of cancer and neurodegenerative diseases.

HDAC6-IN-51 (Compound 7e) is a selective inhibitor of HDAC6, exhibiting an IC50 value of 42.9 nM. This compound demonstrates effective anti-pulmonary fibrosis activity.

HDAC6 ligand-2 (Compound 15) is a ligand of HDAC6 and can be used in the synthesis of PROTAC HDAC6 degrader2.

PROTACHDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader of HDAC6, with an IC50 of 686 nM and a DC50 of 171 nM. It enhances the acetylation of α-tubulin. [Pink: ligand for target protein; Blue: ligand for E3ligaseVHL.]

HDAC6degrader-5 (Compound 6) exhibits inhibitory and degradative activity against HDAC6, with an IC50 of 4.95 nM and a DC50 of 0.96 nM. It suppresses the release of TNF-α, IL-1β, and IL-6, and prevents apoptosis in liver cells. Additionally, HDAC6degrader-5 demonstrates anti-inflammatory properties in a mouse model of APAP-induced liver injury.

HDAC6-IN-52 (EX.1) is a potent HDAC6 inhibitor, achieving a 100% inhibition rate at a concentration of 10 μM. It plays a significant role in central nervous system disorders, including neurodegenerative diseases such as Alzheimer's disease and progressive supranuclear palsy.

PROTAC HDAC6 degrader 2 (Compound 1) is an HDAC6 PROTAC degrader with an IC50 value of 0.643 μM. It facilitates the ubiquitination and degradation of HDAC6 and is applicable in research on hematological and solid cancers.

PD-L1/HDAC6-IN-1 (Compound HP29) is an inhibitor targeting both PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction and inhibiting HDAC6 activity, with IC50 values of 26.8 nM and 69 nM, respectively. This compound enhances the cytotoxicity of Jurkat T cells against HepG2 cells, exhibiting an IC50 of 3.4 μM. In rats, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics, showing a drug exposure level of 871.62 ng·h/mL, and displays antitumor activity in a B16-F10 xenograft mouse model.

PROTAC HDAC6 degrader4 (Compound 17c) is a PROTAC that targets and degrades HDAC6, with a DC50 of 14 nM. It exhibits inhibitory activity against HDAC1, HDAC2, HDAC3, and HDAC6, with IC50 values of 2.2, 2.37, 0.61, and 0.295 μM, respectively. [Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase]

HDAC6ligand-3 serves as a ligand for HDAC6 and can be utilized as a target protein ligand in the synthesis of [PROTAC] HDAC6 degrader4.

HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.

HDAC6-IN-55 (Compound 15B) is a potent HDAC6 inhibitor and an effective anti-inflammatory agent. It mitigates inflammation through the TLR4/MAPK, STAT3, and NF-κB pathways, providing relief from atopic dermatitis. HDAC6-IN-55 alleviates symptoms such as skin edema, dryness, crusting, and peeling in mice with atopic dermatitis induced by 2,4-dinitrochlorobenzene (DNCB).

HDAC6-IN-58 (compound 24c) is a selective HDAC6 inhibitor with IC50 values of 9.5 nM for HDAC6 and 7374.5 nM for HDAC1. It enhances tubulin acetylation, exhibits antiproliferative effects, and induces autophagy (autophagy).

HDAC6-IN-57 (compound 9c) is an HDAC6 inhibitor with an IC50 value of 7 nM. It effectively inhibits 60 different cancer cell lines, with an average GI50 of 2.64 μM, while demonstrating significantly lower cytotoxicity towards non-tumor cell lines.

HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6, with an IC50 of 1.3 nM. This compound can inhibit the S phase and induce apoptosis in HCT-116 colon cancer cells.

HDAC6-IN-60 (Compound 12) is an orally active, selective inhibitor of HDAC6. By inhibiting the enzymatic activity of HDAC6 and modulating pathways related to protein homeostasis, HDAC6-IN-60 affects the proliferation of tumor cells. It holds potential for research in HDAC6-related cancers.

HDAC6-IN-30 (compound 8g) is a selective inhibitor of HDAC6 with an IC50 of 21 nM, and it enhances cellular protein acetylation levels.

HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. It significantly induces apoptosis in B16-F10 cells and causes S phase arrest. Additionally, HDAC6-IN-28 effectively increases the expression of acetylated-α-tubulin both in vitro and in vivo.

HDAC6-IN-29 (compound 11g), an iso-hydroxamic acid derivative, acts as an HDAC6 inhibitor. It shows significant antiproliferative activity against CAL-51 cells (IC50= 1.17 μM) and induces apoptosis, causing cell cycle arrest in the S phase, making it useful for tumor research.

HDAC6-IN-31 (compound 8m) is a selective HDAC6 inhibitor with an IC50 of 0.026 μM. It significantly suppresses the production and release of pro-inflammatory cytokines. HDAC6 plays a crucial role in inhibiting inflammasome activation and holds potential for treating NLRP3 inflammasome-driven inflammatory diseases. Additionally, HDAC6-IN-31 inhibits the migration of glioblastoma cells.

CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1 and HDAC6, with IC50 values of 0.284 μM and 0.6015 μM, respectively. It exhibits antitumor activity.