HDAC Inhibitor

HDAC-IN-59 (compound 13a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-59 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis.

JAK/HDAC-IN-3 (13a) is a dual JAK and HDAC inhibitor, with IC₅₀ values of 25.36 nM, 0.2 μM and 0.43 μM for JAK2, HDAC and HDAC1, respectively.

OKI-005 is an orally active inhibitor of Class I HDACs, with primary targeting of HDAC1, HDAC2 and HDAC3. OKI-005 is a prodrug of OKI-006 (HY-144893). OKI-005 increases histone acetylation levels, induces apoptosis and inhibits cancer cell proliferation. OKI-005 can be used in research related to triple-negative breast cancer and colorectal cancer.

HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC₅₀ values of 0.17, 0.7 and 0.42 μM, respectively.

Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC₅₀ value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

J27644 is a potent HDAC inhibitor. J27644 mitigates TGF-β-induced pulmonary fibrosis.

HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC₅₀ = 0.163 μM and 0.067 μM), and BRD4 (K_i = 0.076 μM), and possess potent antileukemia activity.

FLT3/HDAC-IN-2 is (compound 25h) a FLT3/HDAC dual inhibitor. FLT3/HDAC-IN-2 has antiproliferative activity against MOLM-13 cells. FLT3/HDAC-IN-2 can be used in acute myeloid leukemia research.

HDAC4 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CS4 is a selective HDAC inhibitor with the IC₅₀ values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro.

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

(R)-Dihydrolipoic acid is a compound that inhibits histone deacetylase 6 (HDAC6) activity. The structure of its complex with HDAC6 has been resolved. (R)-Dihydrolipoic acid can inhibit HDAC6 through specific interactions, providing a basis for understanding the relationship between HDAC function and oxidative stress.

Bufexamac (Standard) is the analytical standard of Bufexamac. This product is intended for research and analytical applications. Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 μM and 0.22 μM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.

Valproic acid-d₄ (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC₅₀ values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia.

HDAC6 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

ZYJ-34v is an orally active histone deacetylase inhibitor. ZYJ-34v has antitumor activity.

Vorinostat (GMP) is a GMP grade Vorinosta (HY-10221). GMP-grade small molecules can be used as auxiliary agents in cell therapy. Vorinostat is a potent, orally available HDAC1, HDAC2, HDAC3 (Class I), HDAC6 and Inhibitors of HDAC7 (Class II) and Class IV (HDAC11).

A2AAR/HDAC-IN-2 is a potent A_2AAR/HDAC dual inhibitor, with good binding affinity for A_2AAR (K_i=10.3 nM) and good inhibitory activity against HDAC1 (IC₅₀=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.

anti-TNBC agent-12 (Compound 23a) is a multi-target antitumor agent targeting HDAC6 (IC₅₀=30.3 nM), DNA, and inducing nitric oxide (NO) release. anti-TNBC agent-12 induces tumor cell apoptosis and G2/M phase cell cycle arrest. anti-TNBC agent-12 is promising for research of triple-negative breast cancer (TNBC).