HDAC Inhibitor

1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC₅₀=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.

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.

HDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC₅₀ values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML).

Hdac3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

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.

HDAC6-IN-55 (Compound 15B) is a potent HDAC6 inhibitor and an effective anti-inflammatory agent. HDAC6-IN-55 alleviates atopic dermatitis through anti-inflammatory effects facilitated via TLR4/MAPK, STAT3 and NF-κB pathways. HDAC6-IN-55 alleviates symptoms such as skin edema, dryness, crusting, and peeling in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mice.

Daphnegiravone D (compound 70) is an HDAC6 inhibitor with anti-hepatocellular carcinoma activity. Daphnegiravone D can induce apoptosis and selectively inhibit the proliferation of liver cancer cells through the p38 and JNK MAPK pathways.

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.

HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.

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.

HYF031 is a selective, blood-brain barrier-permeable HDAC8 inhibitor with an IC₅₀ of 5.7 nM, and exhibits extremely low activity against most other HDAC subtypes. HYF031 is applicable for HDAC8 imaging studies.

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

EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC₅₀s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research.

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.

HDAC3-IN-7 (Compound 8ae) is a selective HDAC3 inhibitor with an IC₅₀ value of 311 nM. HDAC3-IN-7 degrades PD-L1 through the lysosome pathway mediated by Cathepsin B, exerting activities such as inhibiting tumor cell proliferation, migration, and invasion. HDAC3-IN-7 is promising for research of cancers.

HDAC-IN-101 is a HDAC1 inhibitor and nitroreductase/pH-activated fluorescent inducer, with an IC₅₀ of 65 nM against human HDAC1. HDAC-IN-101 blocks cancer cell proliferation by inhibiting HDAC1. HDAC-IN-101 is reduced by overexpressed nitroreductase to generate H6AQ (Ex/Em = 450 nm/500 nm), a product that emits fluorescence under low pH conditions. HDAC-IN-101 is applicable for cancer-related research.

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.