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-139815
    ZYJ-34c
    Inhibitor
    ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model.
    ZYJ-34c
  • HY-177441
    Apicidin C
    Inhibitor
    Apicidin C (Compound 5a) is a cyclic tetrapeptide. Apicidin C has an antiprotozoal and antimalarial activity against Eimeria tenella (IC50: 6 nM) by reversibly inhibiting HDAC acyivity. Apicidin C can be used for malaria infections research.
    Apicidin C
  • HY-14842AR
    Givinostat hydrochloride (Standard)
    Inhibitor
    Givinostat (hydrochloride) (Standard) is the analytical standard of Givinostat (hydrochloride). This product is intended for research and analytical applications. Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
    Givinostat hydrochloride (Standard)
  • HY-100585R
    Splitomicin (Standard)
    Inhibitor
    Splitomicin (Standard) is the analytical standard of Splitomicin. This product is intended for research and analytical applications. Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM.
    Splitomicin (Standard)
  • HY-160846
    HDAC6-IN-40
    Inhibitor
    HDAC6-IN-40 (Compound I-6) is an inhibitor for HDAC6 with IC50 of 0.029 μM.
    HDAC6-IN-40
  • HY-128436
    KT-531
    Inhibitor
    KT-531 is a potent and selective inhibitor of HDAC6 with an IC50 of 8.5 nM. KT-531 exhibits strong inhibition against SUP-T11 cells with an IC50 of 0.42 μM. KT-531 can be used in study hematological cancers.
    KT-531
  • HY-W400496
    Valproic acid β-D-glucuronide
    Control
    Valproic acid β-D-glucuronide is the major urinary metabolite of Valproic acid (HY-10585).
    Valproic acid β-D-glucuronide
  • HY-136959
    M133
    Inhibitor
    M133 is a HDAC1 and HDAC2 selective inhibitor which shows potent antiproliferative activity against diverse human tumor cell lines with IC50s of 0.75-1.94 μM. M133 can be used for cancer research.
    M133
  • HY-10225R
    Belinostat (Standard)
    Inhibitor
    Belinostat (Standard) is the analytical standard of Belinostat (HY-10225). This product is intended for research and analytical applications. Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
    Belinostat (Standard)
  • HY-N7036R
    Rhamnetin (Standard)
    Inhibitor
    Rhamnetin (Standard) is the analytical standard of Rhamnetin. This product is intended for research and analytical applications. Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity.
    Rhamnetin (Standard)
  • HY-10528R
    Tasquinimod (Standard)
    Modulator
    Tasquinimod (Standard) is the analytical standard of Tasquinimod. This product is intended for research and analytical applications. Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
    Tasquinimod (Standard)
  • HY-164539
    TMU 35435
    Inhibitor
    TMU 35435 is a histone deacetylase (HDAC) inhibitor. TMU-35435 inhibits the NHEJ pathway through ubiquitination of DNA-dependent protein kinase catalytic subunit (DNA-PKcs). In addition, TMU 35435 enhances radiosensitivity by inducing misfolded protein aggregation and autophagy in TNBC.
    TMU 35435
  • HY-P2178
    Dihydrochlamydocin analog-1
    Inhibitor
    Dihydrochlamydocin analog-1 (compound 2) is a Chlamydocin (HY-115761) analogue that inhibits histone H4 peptide deacetylation with IC50 of 30 nM.
    Dihydrochlamydocin analog-1
  • HY-14842BR
    Givinostat hydrochloride monohydrate (Standard)
    Inhibitor
    Givinostat (hydrochloride monohydrate) (Standard) is the analytical standard of Givinostat (hydrochloride monohydrate). This product is intended for research and analytical applications. Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
    Givinostat hydrochloride monohydrate (Standard)
  • HY-100365R
    Remetinostat (Standard)
    Inhibitor
    Remetinostat (Standard) is the analytical standard of Remetinostat (HY-100365). This product is intended for research and analytical applications. Remetinostat (SHP-141) is a hydroxamic acid-based histone deacetylase (HDAC) inhibitor. Remetinostat alleviates Imiquimod (HY-B0180)-induced psoriatic dermatitis. Remetinostat can be used for study of cutaneous T-cell lymphoma.
    Remetinostat (Standard)
  • HY-12926
    ST7612AA1
    Inhibitor
    ST7612AA1 is a histone deacetylase (HDAC) inhibitor that controls chromatin condensation and DNA transcription by removing acetyl groups from histones. ST7612AA1 is also a potent HIV reactivation inducer, and its reactivation activity is exerted without activating or proliferating CD4+T cells, and can be used in the study of HIV reactivation strategies and elimination of viral reservoirs.
    ST7612AA1
  • HY-176545
    Z-MAL
    Substrate
    Z-MAL is a highly efficient and broad-spectrum HDAC substrate. Z-MAL exhibits high conversion activity for class I, II histone deacetylases, and class III SIRT1. Z-MAL can be used in studies on the structure-activity relationship, subtype selectivity, and inhibitor screening of HDAC.
    Z-MAL
  • HY-W555601
    Nicoxamat
    Inhibitor 99.05%
    Nicoxamat (N-Hydroxynicotinamide) is a HCV inhibitor as well as a selective HDAC6 inhibitor. Nicoxamat is applicable to research related to hepatitis C virus (HCV) infection.
    Nicoxamat
  • HY-181010
    HDAC1-IN-12
    Inhibitor
    HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC50 of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H3 acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria.
    HDAC1-IN-12
  • HY-172167
    PD-L1/HDAC-IN-1
    Inhibitor
    PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC50 of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC50=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME.
    PD-L1/HDAC-IN-1
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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