1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Epigenetics
  3. HDAC

HDAC

Histone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on ahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-136859
    BATCP
    Inhibitor 99.77%
    BATCP is a HDAC (Histone deacetylases) inhibitor.
    BATCP
  • HY-139122
    Butyrylhydroxamic acid
    Inhibitor
    Butyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histone deacetylase (HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies.
    Butyrylhydroxamic acid
  • HY-111028
    J1038
    Inhibitor
    J1038 (T 5979345) is a selective HDAC8 inhibitor. J1038 binds the catalytic zinc ion of Schistosoma mansoni HDAC8 (smHDAC8).
    J1038
  • HY-100871R
    WT-161 (Standard)
    Inhibitor
    WT-161 (Standard) is the analytical standard of WT-161 (HY-100871). This product is intended for research and analytical applications. WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    WT-161 (Standard)
  • HY-104008R
    ACY-957 (Standard)
    Inhibitor
    ACY-957 (Standard) is the analytical standard of ACY-957 (HY-104008). This product is intended for research and analytical applications. ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.
    ACY-957 (Standard)
  • HY-14842R
    Givinostat (Standard)
    Inhibitor
    Givinostat (Standard) is the analytical standard of Givinostat. This product is intended for research and analytical applications. Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat can be used for Duchenne muscular dystrophy (DMD) research.
    Givinostat (Standard)
  • HY-18613R
    CAY10603 (Standard)
    Inhibitor
    CAY10603 (Standard) is the analytical standard of CAY10603. This product is intended for research and analytical applications. CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
    CAY10603 (Standard)
  • HY-16026R
    Ricolinostat (Standard)
    Inhibitor
    Ricolinostat (Standard) is the analytical standard of Ricolinostat. This product is intended for research and analytical applications. Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
    Ricolinostat (Standard)
  • HY-106409R
    Tefinostat (Standard)
    Inhibitor
    Tefinostat (Standard) is the analytical standard of Tefinostat (HY-106409). This product is intended for research and analytical applications. Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.
    Tefinostat (Standard)
  • HY-169923
    HDAC-IN-83
    Inhibitor
    HDAC-IN-83 (compound 9D) is an inhibitor of deacetylases (HDACs) (IC50=0.01 μM/0.44 μM HDAC1/HDAC6) with anticancer, antiproliferative and caspase 3/7 activation activities. HDAC-IN-83 inhibits Cal27, HepG2 and MRC-5 with IC50s of 0.693 μM, 0.427 μM and 3.19 μM, respectively.
    HDAC-IN-83
  • HY-P2044
    Azumamide E
    Inhibitor
    Azumamide E is a HDAC inhibitor, with an IC50 of 0.064 μM against HDAC, 1.22 μM against HDAC1, and 2.28 μM against HDAC4. Azumamide E inhibits HDAC activity in nuclear extracts of leukemia cells and cervical adenocarcinoma cells. Azumamide E suppresses angiogenesis. Azumamide E is applicable for research on leukemia, cervical adenocarcinoma, and anti-angiogenesis.
    Azumamide E
  • HY-169922
    HDAC-IN-82
    Inhibitor
    HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin.
    HDAC-IN-82
  • HY-13271R
    Tubastatin A Hydrochloride (Standard)
    Inhibitor
    Tubastatin A (Hydrochloride) (Standard) is the analytical standard of Tubastatin A (Hydrochloride). This product is intended for research and analytical applications. Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    Tubastatin A Hydrochloride (Standard)
  • HY-180343
    FFK29
    Inhibitor
    FFK29 is a synthetic class II histone deacetylase inhibitor (HDACi). FFK29 can potently inhibit the growth and encystation of Acanthamoeba. FFK29 can be studied in research on protozoan and parasitic diseases.
    FFK29
  • HY-N14950
    Diheteropeptin
    Inhibitor
    Diheteropeptin has similar activity to T ransforming growth factor-β, and inhibits the ability of HDAC.
    Diheteropeptin
  • HY-13271AR
    Tubastatin A (Standard)
    Inhibitor
    Tubastatin A (Standard) is the analytical standard of Tubastatin A. This product is intended for research and analytical applications. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    Tubastatin A (Standard)
  • HY-10226R
    JNJ-16241199 (Standard)
    Inhibitor
    JNJ-16241199 (Standard) is the analytical standard of JNJ-16241199 (HY-10226). This product is intended for research and analytical applications. JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.
    JNJ-16241199 (Standard)
  • HY-185554A
    (S)-HDAC-IN-102
    Inhibitor
    (S)-HDAC-IN-102 is a HDAC8 inhibitor and an isomer of HDAC-IN-102 (HY-185554). HDAC-IN-102 inhibits total HDAC with an IC50 of 58 μM and exhibits partial subtype selectivity. Specifically, (S)-HDAC-IN-102 targets HDAC8, while (R)-HDAC-IN-102 (HY-185554B) targets HDAC2. HDAC-IN-102 exerts antioxidant effects by scavenging DPPH free radicals and can be used in cancer-related research.
    (S)-HDAC-IN-102
  • HY-10223R
    CUDC-101 (Standard)
    Inhibitor
    CUDC-101 (Standard) is the analytical standard of CUDC-101 (HY-10223). This product is intended for research and analytical applications. CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CUDC-101 (Standard)
  • HY-160845
    HDAC6-IN-39
    Inhibitor
    HDAC6-IN-39 (Compound I-132) is an inhibitor for HDAC6 with IC50 of 0.0096 μM.
    HDAC6-IN-39
Cat. No. Product Name / Synonyms Application Reactivity

TCR, GPCR and HDAC II interaction: Diverse agonists act through G-protein-coupled receptors (GPCRs) to activate the PKC-PKD axis, CaMK, Rho, or MHC binding to antigens stimulates TCR to activate PKD, leading to phosphorylation of class II HDACs. Phospho-HDACs dissociate from MEF2, bind 14-3-3, and are exported to the cytoplasm through a CRM1-dependent mechanism. CRM1 is inhibited by leptomycin B (LMB). Release of MEF2 from class II HDACs allows p300 to dock on MEF2 and stimulate gene expression. Dephosphorylation of class II HDACs in the cytoplasm enables reentry into the nucleus[1].

 

TLR: TLR signaling is initiated by ligand binding to receptors. The recruitment of TLR domain-containing adaptor protein MyD88 is repressed by HDAC6, whereas NF-κB and MTA-1 can be negatively regulated by HDAC1/2/3 and HDAC2, respectively. Acetylation by HATs enhance MKP-1 which inhibits p38-mediated inflammatory responses, while HDAC1/2/3 inhibits MKP-1 activity. HDAC1 and HDAC8 repress, whereas HDAC6 promotes, IRF function in response to viral challenge. HDAC11 inhibits IL-10 expression and HDAC1 and HDAC2 represses IFNγ-dependent activation of the CIITA transcription factor, thus affecting antigen presentation[2][3].

 

IRNAR: IFN-α/β induce activation of the type I IFN receptor and then bring the receptor-associated JAKs into proximity. JAK adds phosphates to the receptor. STATs bind to the phosphates and then phosphorylated by JAKs to form a dimer, leading to nuclear translocation and gene expression. HDACs positively regulate STATs and PZLF to promote antiviral responses and IFN-induced gene expression[2][3].

 

Cell cycle: In G1 phase, HDAC, Retinoblastoma protein (RB), E2F and polypeptide (DP) form a repressor complex. HDAC acts on surrounding chromatin, causing it to adopt a closed chromatin conformation, and transcription is repressed. Prior to the G1-S transition, phosphorylation of RB by CDKs dissociates the repressor complex. Transcription factors (TFs) gain access to their binding sites and, together with the now unmasked E2F activation domain. E2F is then free to activate transcription by contacting basal factors or by contacting histone acetyltransferases, such as CBP, that can alter chromatin structure[4].

 

The function of non-histone proteins is also regulated by HATs/HDACs. p53: HDAC1 impairs the function of p53. p53 is acetylated under conditions of stress or HDAC inhibition by its cofactor CREB binding protein (CBP) and the transcription of genes involved in differentiation is activated. HSP90: HSP90 is a chaperone that complexes with other chaperones, such as p23, to maintain correct conformational folding of its client proteins. HDAC6 deacetylates HSP90. Inhibition of HDAC6 would result in hyperacetylated HSP90, which would be unable to interact with its co-chaperones and properly lead to misfolded client proteins being targeted for degradation via the ubiquitin-proteasome system[5][6].
 

Reference:

[1]. Vega RB, et al. Protein kinases C and D mediate agonist-dependent cardiac hypertrophy through nuclear export of histone deacetylase 5.Mol Cell Biol. 2004 Oct;24(19):8374-85.
[2]. Shakespear MR, et al. Histone deacetylases as regulators of inflammation and immunity. Trends Immunol. 2011 Jul;32(7):335-43.
[3]. Suliman BA, et al. HDACi: molecular mechanisms and therapeutic implications in the innate immune system.Immunol Cell Biol. 2012 Jan;90(1):23-32. 
[4]. Brehm A, et al. Retinoblastoma protein meets chromatin.Trends Biochem Sci. 1999 Apr;24(4):142-5.
[5]. Butler R, et al. Histone deacetylase inhibitors as therapeutics for polyglutamine disorders.Nat Rev Neurosci. 2006 Oct;7(10):784-96
[6]. Minucci S, et al. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer.Nat Rev Cancer. 2006 Jan;6(1):38-51.

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