HDAC Inhibitor

HPO-DAEE (4-Hydroperoxy-2-decenoic acid ethyl ester) elicits nuclear accumulation of Nrf2 and activated antioxidant response element (ARE). HPO-DAEE induces antioxidant genes upregulation (eg: HO-1) through Nrf2-ARE signaling. HPO-DAEE induces reactive oxygen species generation. HPO-DAEE also inhibits histone deacetylase and upregulate expression of extracellular superoxide dismutase via histone acetylation. HPO-DAEE protects against 6-hydroxydopamine-induced cell death via activation of Nrf2-ARE and eIF2α-ATF4 pathways.

HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC₅₀s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI₅₀ of 0.32 and 1.1 μM respectively.

c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC₅₀ value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G₀/G₁ phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines.

Fimepinostat mesylate potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC₅₀ of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

PTERi is a selective inhibitor of PTER with selectivity towards HDACs. PTERi increases the level of N-acetyltaurine in both lean and obese mice, and reduces food intake in obese mice. PTERi can be used in the research of obesity.

Hdac4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hdac4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.

HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu²⁺-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue.

HDAC-IN-61 (compound 12k) is a potent and orally active HDAC inhibitor. HDAC-IN-61 has anticancer active with an IC₅₀ value of 30 nM for Bel-7402 cell. HDAC-IN-61 can be used in research of cancer.

W2A-28 is a daul modulator of class I HDACs and Wnt/β-catenin. W2A-28 inhibits HDAC1, 2 and 3 activities with IC₅₀ values of 512, 675, and 217 nM, respectively. W2A-28 shows selectivity over other HDACs and Sirtuin family members. W2A-28 activates Wnt/β-catenin signaling via reduced LRP6 degradation, enhances histone acetylation, suppresses tau phosphorylation, and reduces Aβ₄₀ and Aβ₄₂ levels. W2A-28 can be used for the research of Alzheimer's disease.

PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC₅₀s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6). br/.

HDAC-IN-102 (Compound 21) is a histone deacetylase (HDAC) inhibitor with an IC₅₀ of 58 μM. HDAC-IN-102 inhibits total HDAC activity and exhibits partial subtype selectivity, with the R-isomer targeting HDAC2 and the S-isomer targeting HDAC8. HDAC-IN-102 exerts antioxidant effects by scavenging DPPH free radicals. HDAC-IN-102 can be used in cancer-related research.

WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer.

HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity.

MFDCH016 is a potent HDAC1/6 (IC₅₀ = 38/59 nM) and CDK4/6 (IC₅₀ = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer.

JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC₅₀ values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity.

HDAC-IN-78 (compound 66a) is a HDAC inhibitor. HDAC-IN-78 can be used in cancer research.

BChE/HDAC6-IN-2 (compound 29a) is a dual inhibitor of BChE and HDAC6 with IC₅₀s of 1.8 nM and 71.0 nM, respectively. BChE/HDAC6-IN-2 has prominently neuroprotective effects and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is also an effective chelator of metal ion (Fe²⁺ and Cu²⁺). BChE/HDAC6-IN-2 inhibits phosphorylation of tau, and exhibits moderate immunomodulatory effect.

CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC₅₀ values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model.

HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research.