HDAC

Histone deacetylase (HDAC) inhibitors block enzymes that remove acetyl groups from histones and other proteins. Deacetylation compacts chromatin and generally represses transcription, so HDAC inhibitors are widely used to study gene regulation. Trichostatin A was characterized in 1990 as a specific inhibitor of mammalian histone deacetylase. The first mammalian HDAC was cloned in 1996 and found to be related to the yeast transcriptional regulator Rpd3p. Isoform-selective tools include entinostat for HDAC1 and HDAC3, and Tubastatin A HCl for HDAC6, a microtubule-associated deacetylase. Broad-spectrum hydroxamates such as vorinostat and panobinostat, together with the cyclic depsipeptide romidepsin, complete the range.

16 Items

  • J22352
    Cat. No.
    A19174

    J22352

    J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM.

    2 mg
    $45.00
    5 mg
    $100.00
    All 5 sizes
  • JPS016 TFA
    Cat. No.
    A23951

    JPS016 TFA

    JPS016 is a benzamide-based PROTAC that recruits the Von Hippel-Lindau (VHL) E3 ligase to selectively degrade class I histone deacetylases (HDACs). It is a potent degrader of HDAC1/2, leading to broad transcriptional changes and enhanced apoptosis in HCT116 cells, supporting its application in epigenetic and cancer research.

    1 mg
    $144.00
    5 mg
    $432.00
    All 4 sizes
  • YX968
    Cat. No.
    A24008

    YX968

    YX968 is a potent and selective PROTAC degrader targeting histone deacetylases HDAC3 and HDAC8, with DC₅₀ values of 1.7 nM and 6.8 nM, respectively. By inducing degradation of these epigenetic regulators, YX968 promotes apoptosis and exhibits significant antitumor activity, representing a promising therapeutic strategy for cancers driven by aberrant HDAC3/8 activity.

    1 mg
    $252.00
    2 mg
    $434.00
    All 4 sizes
  • JPS014
    Cat. No.
    A26348

    JPS014

    JPS014 is a benzamide-based HDAC degrader designed to engage the Von Hippel-Lindau (VHL) E3 ligase for targeted proteolysis. It effectively degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression profiles and promoting apoptotic pathways in HCT116 cancer cells. This compound is particularly useful for studying the role of HDAC inhibition in cancer biology and elucidating mechanisms of resistance to therapies.

    Out of stock

    All 3 sizes
  • HDAC6 degrader-4
    Cat. No.
    A26366

    HDAC6 degrader-4

    HDAC6 degrader-4 is a PROTAC that selectively targets and degrades HDAC6. By combining a non-selective HDAC inhibitor with a thalidomide-type E3 ligase ligand, it effectively modulates histone deacetylation. This reagent is primarily utilized in cancer research to investigate the role of HDAC6 in tumor progression and to evaluate potential therapeutic strategies.

    1 mg
    $285.00
    5 mg
    $735.00
    All 3 sizes
  • PROTAC HDAC4 Degrader-1
    Cat. No.
    A26404

    PROTAC HDAC4 Degrader-1

    PROTAC HDAC4 Degrader-1 is a selective PROTAC that targets and promotes the degradation of HDAC4, a histone deacetylase involved in regulating gene expression. This compound effectively decreases HDAC4 protein levels, leading to S phase cell cycle arrest and reduced tumor cell proliferation, as evidenced by its impact on colony formation. Additionally, PROTAC HDAC4 Degrader-1 demonstrates efficacy in vivo in H460 mouse models, making it a valuable tool for cancer research, particularly in studies related to lung cancer.

    Out of stock

    All 3 sizes
  • YX862
    Cat. No.
    A26423

    YX862

    YX862 is a selective PROTAC degrader targeting HDAC8, designed to induce robust degradation of this histone deacetylase. It achieves over 95% degradation of HDAC8 at a concentration of 250 nM in MDA-MB-231 cells. This compound serves as a valuable tool for investigating the role of HDAC8 in various biological processes and provides insights into potential therapeutic strategies for HDAC8-related diseases.

    5 mg
    $600.00
    10 mg
    $985.00
    All 4 sizes
  • JPS035
    Cat. No.
    A26482

    JPS035

    JPS035 is a benzamide-derived HDAC degrader that utilizes the Von Hippel-Lindau (VHL) E3 ligase-mediated PROTAC technology. It specifically targets and degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression and promoting apoptosis in HCT116 colorectal cancer cells. This compound serves as a valuable tool for studies focused on epigenetic modulation and therapeutic strategies against HDAC-related diseases.

    Out of stock

    All 3 sizes
  • JPS016
    Cat. No.
    A26487

    JPS016

    JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction.

    5 mg
    $710.00
    All 1 sizes
  • HD-TAC7
    Cat. No.
    A26537

    HD-TAC7

    HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD).

    1 mg
    $160.00
    5 mg
    $375.00
    All 6 sizes
  • JPS036
    Cat. No.
    A26550

    JPS036

    JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models.

    1 mg
    $280.00
    5 mg
    $710.00
    All 2 sizes
  • SZUH280
    Cat. No.
    A30796

    SZUH280

    SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation.

    5 mg
    $280.00
    10 mg
    $460.00
    All 5 sizes
  • JPS004
    Cat. No.
    A32036

    JPS004

    JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications.

    Out of stock

    All 3 sizes
  • PROTAC HDAC6 degrader 1
    Cat. No.
    A32174

    PROTAC HDAC6 degrader 1

    PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways.

    Out of stock

    All 3 sizes
  • HDAC6 degrader-5
    Cat. No.
    A64893

    HDAC6 degrader-5

    HDAC6 degrader-5 functions as an HDAC6 degrader, demonstrating potent inhibitory and degradation capabilities with an IC50 of 4.95 nM and a DC50 of 0.96 nM. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, while also preventing hepatocyte apoptosis. Additionally, HDAC6 degrader-5 shows anti-inflammatory effects in mouse models of acetaminophen-induced liver injury, making it a valuable tool for research on inflammatory diseases and liver pathologies.

    5 mg
    $305.00
    10 mg
    $540.00
    All 5 sizes
  • HDAC3 degrader-2
    Cat. No.
    A64899

    HDAC3 degrader-2

    HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions.

    Out of stock

    All 3 sizes

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